hDDAH-1-IN-2 sulfate

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

hDDAH-1-IN-2 sulfate 

hDDAH-1-IN-2 是一种选择性、具有口服活性的人二甲基精氨酸二甲基氨基水合-1 (hDDAH-1)。hDDAH-1-IN-2 对细胞毒性/活力良好。

hDDAH-1-IN-2 sulfate

hDDAH-1-IN-2 sulfate Chemical Structure

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生物活性

hDDAH-1-IN-2 is a selective, orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor. hDDAH-1-IN-2 reveals an excellent profile regarding cell toxicity/viability[1].

分子量

400.43

Formula

C8H24N4O10S2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Lunk I, et al. Discovery of N-(4-Aminobutyl)-N’-(2-methoxyethyl)guanidine as the First Selective, Nonamino Acid, Catalytic Site Inhibitor of Human Dimethylarginine Dimethylaminohydrolase-1 (hDDAH-1).J Med Chem. 2020 Jan 9;63(1):425-432.

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Bleomycin Sulfate

Bleomycin Sulfate

Popular Antibiotics
10mM in DMSO

有货

Bleomycin Sulfate

CAS编号 9041-93-4(DMSO) | 品牌:Jinpan
Bleomycin (NSC125066) sulfate

MSDS

质检证书(CoA)

相似产品

  • 分子式 C55H85N17O25S4
  • 分子量1512.62

货号 (SKU) 包装规格 是否现货 价格 数量
B408760-1ml 1ml 期货 Bleomycin Sulfate  

基本信息

产品名称 Bleomycin Sulfate
英文名称 Bleomycin (NSC125066) sulfate
规格或纯度 10mM in DMSO
运输条件 超低温冰袋运输
生化机理 Bleomycin Sulfate (NSC125066) is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells.

一般描述

Information

Bleomycin Sulfate (NSC125066) is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells.
In vitro

UT-SCC-12A and UT-SCC-12B are both more resistant to Bleomycin sulfate with IC50 of 14.2 nM and 13 nM, respectively. Alveolar macrophages incubated with 0.01 μg/mL to 1μg /mL Bleomycin sulfate for 18 hours secretes significantly more fibroblast growth factor than macrophages incubated without Bleomycin sulfate. Macrophages stimulated with Bleomycin sulfate continues to produce significant amounts of fibroblast growth factor even after Bleomycin sulfate is removed and replaced with fresh (Bleomycin sulfate-free) media. Fibroblast growth factor secretion by Bleomycin sulfate-stimulated alveolar macrophages is inhibited by cycloheximide, and the 5-lipoxygenase inhibitors NDGA (nordihydroguaiaretic acid) and BW755c, indicating not only a requirement for protein synthesis but also for metabolites of the 5-lipoxygenase pathway of arachidonic acid metabolism for full expression of activity. Bleomycin sulfate (400 µg/mL) incubation for 24 hours decreases the viability of NTera-2 cells, and increases caspase-3, -8 and -9 activities, Bax and cytoplasmic cytochrome c levels and decreases Bcl-2 levels. In terms of unstable aberrations, the clastogenic effect of Bleomycin sulfate on ADIPO-P2 cells persists for at least 10 days after exposure. Bleomycin sulfate-induced telomere instability in mammalian cells persists for several generations after exposure. Moreover, the appearance of telomere fusions in Bleomycin sulfate-exposed cells 10 days after treatment suggests that Bleomycin sulfate can induce delayed telomere instability.

In vivo

Day 7 post-Bleomycin sulfate, CD45+ cells in BALf in NOX-/- is 1.7-fold > WT, 57% of which are Mf that decreases by 67% in WT and 83% in NOX-/- by Day 21.
Cell Data

cell lines:

Concentrations:2.5 μg/mL

Incubation Time:30 minutes

Powder Purity:≥98%

Information

Bleomycin Sulfate (NSC125066) is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells.
In vitro

UT-SCC-12A and UT-SCC-12B are both more resistant to Bleomycin sulfate with IC50 of 14.2 nM and 13 nM, respectively. Alveolar macrophages incubated with 0.01 μg/mL to 1μg /mL Bleomycin sulfate for 18 hours secretes significantly more fibroblast growth factor than macrophages incubated without Bleomycin sulfate. Macrophages stimulated with Bleomycin sulfate continues to produce significant amounts of fibroblast growth factor even after Bleomycin sulfate is removed and replaced with fresh (Bleomycin sulfate-free) media. Fibroblast growth factor secretion by Bleomycin sulfate-stimulated alveolar macrophages is inhibited by cycloheximide, and the 5-lipoxygenase inhibitors NDGA (nordihydroguaiaretic acid) and BW755c, indicating not only a requirement for protein synthesis but also for metabolites of the 5-lipoxygenase pathway of arachidonic acid metabolism for full expression of activity. Bleomycin sulfate (400 µg/mL) incubation for 24 hours decreases the viability of NTera-2 cells, and increases caspase-3, -8 and -9 activities, Bax and cytoplasmic cytochrome c levels and decreases Bcl-2 levels. In terms of unstable aberrations, the clastogenic effect of Bleomycin sulfate on ADIPO-P2 cells persists for at least 10 days after exposure. Bleomycin sulfate-induced telomere instability in mammalian cells persists for several generations after exposure. Moreover, the appearance of telomere fusions in Bleomycin sulfate-exposed cells 10 days after treatment suggests that Bleomycin sulfate can induce delayed telomere instability.

In vivo

Day 7 post-Bleomycin sulfate, CD45+ cells in BALf in NOX-/- is 1.7-fold > WT, 57% of which are Mf that decreases by 67% in WT and 83% in NOX-/- by Day 21.
Cell Data

cell lines:

Concentrations:2.5 μg/mL

Incubation Time:30 minutes

Powder Purity:≥98%

相关属性

CAS编号 9041-93-4(DMSO)
储存温度 -80℃储存
分子量 1512.62
分子式 C55H85N17O25S4
品牌 Jinpan
Smiles CC(O)C(NC(=O)C(C)C(O)C(C)NC(=O)C(NC(=O)C1=C(C)C(=NC(=N1)C(CC(N)=O)NCC(N)C(N)=O)N)C(OC2OC(CO)C(O)C(O)C2OC3OC(CO)C(O)C(OC(N)=O)C3O)C4=C[NH]C=N4)C(=O)NCCC5=NC(=CS5)C6=NC(=CS6)C(=O)NCCC[S+](C)C.O[S]([O-])(=O)=O

Capreomycin sulfate

Capreomycin sulfate

环肽抗生素属于结核菌素家族的抗生素。
10mM in Water

有货

Capreomycin sulfate

CAS编号 1405-37-4 | 品牌:Jinpan
Capreomycin sulfate

MSDS

质检证书(CoA)

相似产品

  • 分子式 C25H44N14O7.H2SO4
  • 分子量750.78
  • EC号 215-776-8
  • PubChem编号 22836615

货号 (SKU) 包装规格 是否现货 价格 数量
C421518-1ml 1ml 期货 Capreomycin sulfate  

基本信息

产品名称 Capreomycin sulfate
英文名称 Capreomycin sulfate
别名 硫酸卷曲霉素
英文别名 Capreomycin sulfate salt
规格或纯度 10mM in Water
运输条件 超低温冰袋运输
生化机理 环肽抗生素被认为可以通过结合70S核糖体单位来抑制蛋白质合成。破坏结核分枝杆菌核糖体蛋白L12和L10的相互作用。

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

相关属性

CAS编号 1405-37-4
沸点 1377℃
储存温度 -80℃储存
RTECS EX8930000
分子量 750.78
分子式 C25H44N14O7.H2SO4
EC号 215-776-8
品牌 Jinpan
PubChem CID 22836615

Cas(1405-37-4), Capreomycin sulfate, 硫酸卷曲霉素,Capreomycin sulfate,

硫酸卷曲霉素

环肽抗生素属于结核菌素家族的抗生素。
Potency 700 – 1050 μG/mg

有货

Cas(1405-37-4), Capreomycin sulfate, 硫酸卷曲霉素,Capreomycin sulfate,

CAS编号 1405-37-4 | 品牌:Jinpan
Capreomycin sulfate

MSDS

质检证书(CoA)

相似产品

  • 分子式 C25H44N14O7.H2SO4
  • 分子量750.78
  • EC号 215-776-8
  • MDL号 MFCD00079032
  • PubChem编号 22836615

货号 (SKU) 包装规格 是否现货 价格 数量
C117924-100mg 100mg 现货 Cas(1405-37-4), Capreomycin sulfate, 硫酸卷曲霉素,Capreomycin sulfate,  
C117924-500mg 500mg 现货 Cas(1405-37-4), Capreomycin sulfate, 硫酸卷曲霉素,Capreomycin sulfate,  
C117924-1g 1g 现货 Cas(1405-37-4), Capreomycin sulfate, 硫酸卷曲霉素,Capreomycin sulfate,  
C117924-5g 5g 现货 Cas(1405-37-4), Capreomycin sulfate, 硫酸卷曲霉素,Capreomycin sulfate,  
C117924-25g 25g 现货 Cas(1405-37-4), Capreomycin sulfate, 硫酸卷曲霉素,Capreomycin sulfate,  

基本信息

产品名称 硫酸卷曲霉素
英文名称 Capreomycin sulfate
别名 硫酸卷曲霉素
英文别名 Capreomycin sulfate salt
规格或纯度 Potency 700 – 1050 μG/mg
运输条件 超低温冰袋运输
生化机理 环肽抗生素被认为可以通过结合70S核糖体单位来抑制蛋白质合成。破坏结核分枝杆菌核糖体蛋白L12和L10的相互作用。

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.Capreomycin是多肽类抗生素,与其它抗生素结合用于MDR-肺结核。

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

相关属性

CAS编号 1405-37-4
沸点 1377℃
溶解性 Freely soluble in water
储存温度 -20°C储存
RTECS EX8930000
MDL号 MFCD00079032
密度 1.34
分子量 750.78
分子式 C25H44N14O7.H2SO4
EC号 215-776-8
品牌 Jinpan
备注 如果有可能,您尽量在同一天配置溶液,并在当天使用完它。但是,如果您需要预先配制储备溶液,我们建议您将溶液等份保存在-20°C的密封小瓶中。通常,它们最多可以使用一个月。在使用前和打开样品瓶之前,我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
PubChem CID 22836615

GC7 Sulfate

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

GC7 Sulfate  纯度: ≥98.0%

GC7 Sulfate 是一种脱氧嘌呤合成酶 (DHPS) 抑制剂。

GC7 Sulfate

GC7 Sulfate Chemical Structure

CAS No. : 150417-90-6

规格 价格 是否有货 数量
10 mM * 1 mL in Water ¥1640 In-stock
1 mg ¥550 In-stock
5 mg ¥1650 In-stock
10 mg ¥2600 In-stock
25 mg ¥5200 In-stock
50 mg ¥8300 In-stock
100 mg ¥13200 In-stock
200 mg   询价  
500 mg   询价  

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GC7 Sulfate 相关产品

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生物活性

GC7 Sulfate is a deoxyhypusine synthase (DHPS) inhibitor.

IC50 & Target

DHPS[1]

体外研究
(In Vitro)

The treatment of MYCN2 (±Dox) and BE(2)-C cells with GC7 Sulfate for 72 h at various concentrations (0.1 to 100 μM) significantly reduces the number of viable cells in a dose-dependent manner. In MYCN2 cells, 5 μM of GC7 Sulfate inhibits cell viability by ~40 and ~60 %, respectively, compare to untreated control cells. BE(2)-C cells require 25 μM of GC7 Sulfate to reduce cell viability by ~50 %. Exposure to 10 and 100 μM GC7 for 72 h clearly decreases the levels of total retinoblastoma (Rb) and phosphorylated Rb as well as of Cdk4 protein, and increases the levels of p21 protein[1]. Between 0 and 20 μM, GC7 Sulfate induces little cytotoxicity in HCC cells, while higher concentrations of GC7 Sulfate (50 to 100 μM) significantly inhibit the viability of all five HCC cell lines tested. Newly synthesized 3H-labeled hypusine of eIF5A1/eIF5A2 is rarely detected after 20 μM GC7 Sulfate treatment, compare to untreated control. The activity of [3H]-spermidine incorporated into HCC cells is significantly decreased by 20 μM GC7 Sulfate or higher concentration[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

270.35

Formula

C8H22N4O4S

CAS 号

150417-90-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 3 mg/mL (11.10 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6989 mL 18.4945 mL 36.9891 mL
5 mM 0.7398 mL 3.6989 mL 7.3978 mL
10 mM 0.3699 mL 1.8495 mL 3.6989 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Bandino A, et al. Deoxyhypusine synthase (DHPS) inhibitor GC7 induces p21/Rb-mediated inhibition of tumor cell growth and DHPS expression correlates with poor prognosis in neuroblastoma patients. Cell Oncol (Dordr). 2014 Dec;37(6):387-98.

    [2]. Lou B, et al. N1-guanyl-1,7-diaminoheptane (GC7) enhances the therapeutic efficacy of doxorubicin by inhibiting activation of eukaryotic translation initiation factor 5A2 (eIF5A2) and preventing the epithelial-mesenchymal transition in hepatocellular carcinoma cells. Exp Cell Res. 2013 Oct 15;319(17):2708-17.

Cell Assay
[1]

Cell viability is analyzed with the MTS assay kit in accordance with the manufacturer’s protocols. Briefly, after treatment with GC7 Sulfate for 72 h at various concentrations (0.1 to 100 μM) in 96-well plates, cells are directly incubated with the MTS dye reagent for 1 h at 37°C in a 5 % CO2 atmosphere. The absorbance is read at 490 nm using a reader[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Bandino A, et al. Deoxyhypusine synthase (DHPS) inhibitor GC7 induces p21/Rb-mediated inhibition of tumor cell growth and DHPS expression correlates with poor prognosis in neuroblastoma patients. Cell Oncol (Dordr). 2014 Dec;37(6):387-98.

    [2]. Lou B, et al. N1-guanyl-1,7-diaminoheptane (GC7) enhances the therapeutic efficacy of doxorubicin by inhibiting activation of eukaryotic translation initiation factor 5A2 (eIF5A2) and preventing the epithelial-mesenchymal transition in hepatocellular carcinoma cells. Exp Cell Res. 2013 Oct 15;319(17):2708-17.

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L-Canavanine sulfate

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

L-Canavanine sulfate  纯度: ≥98.0%

L-Canavanine sulfate 是诱导型 NO 合酶 (NO synthase) 的选择性抑制剂。

L-Canavanine sulfate

L-Canavanine sulfate Chemical Structure

CAS No. : 2219-31-0

规格 价格 是否有货 数量
10 mM * 1 mL in Water ¥550 In-stock
50 mg ¥500 In-stock
100 mg ¥700 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

L-Canavanine sulfate 相关产品

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  • Targeted Diversity Library

生物活性

L-Canavanine sulfate is a selective inhibitor of inducible NO synthase.

IC50 & Target

NO synthase[1]

体外研究
(In Vitro)

L-Canavanine sulfate (L-CAV) causes only a limited degree of cytotoxicity in HeLa, Hep G2, and SK-HEP-1 cells when given alone in arginine-rich media with IC50 values ranging from 5 to 10 mM. In HaCaT keratinocyte cell line, IC50 of L-Canavanine sulfate exceeds the concentration of 10 mM, indicating low cytotoxicity in normal cells in vitro. In arginine-free media, IC50 of L-Canavanine sulfate in HeLa, Hep G2, and SK-HEP-1 cells are 0.21±0.04; 0.64±0.16; and 1.18±0.14 mM, respectively. L-Canavanine sulfate, which is hardly toxic alone, potentiates the cytotoxicity of vinblastine (VIN) and paclitaxel (PTX) in HeLa and hepatocellular carcinoma cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Administration of L-Canavanine sulfate (100 mg/kg) produces a moderate increase in mean arterial pressure of 20 mm Hg, returns blood pressure to near basal levels and completely attenuates the lipopolysaccharide-induced hypotension. All, but one, endotoxaemic rats dosed with L-Canavanine sulfate (100 mg/kg) survive for 6 h post lipopolysaccharide, after which time the experiment is terminated (n=7)[1]. L-canavanine inhibits DNA synthesis by Li 210 cells in vivo and significantly increases the lifespan of animals bearing the Li 210 leukemia. An optimal dose of 18 g/kg produces a peak increase in lifespan of 44%. The therapeutic dose range is narrow, and a dose of 24 g/kg causes death due to drug toxicity[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

274.25

Formula

C5H14N4O7S

CAS 号

2219-31-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 100 mg/mL (364.63 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6463 mL 18.2315 mL 36.4631 mL
5 mM 0.7293 mL 3.6463 mL 7.2926 mL
10 mM 0.3646 mL 1.8232 mL 3.6463 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Teale DM, et al. L-canavanine restores blood pressure in a rat model of endotoxic shock. Eur J Pharmacol. 1994 Dec 12;271(1):87-92.

    [2]. Nurcahyanti AD, et al. Cytotoxic potentiation of vinblastine and paclitaxel by L-canavanine in human cervical cancer and hepatocellular carcinoma cells. Phytomedicine. 2015 Dec 15;22(14):1232-7.

    [3]. Green MH, et al. Antitumor activity of L-canavanine against L1210 murine leukemia. Cancer Res. 1980 Mar;40(3):535-7.

Cell Assay
[2]

A dose-dependent cytotoxicity is examined using the MTT assay. Into each well of 96-well plates, 2×104 of cells are seeded, and after 24 h incubation, cells are incubated with test compounds (including L-Canavanine sulfate). After 24 h, 0.5 mg/mL of MTT is added to each well of HeLa, Caco-2, MIA PaCa-2, BxPC-3 and SK-HEP-1 cells, while MTT is added to Hep G2 after 48 h incubation with test compounds (including L-Canavanine sulfate). The cells are then incubated for 3 h so that the viable cells could produce formazan crystals; they are then dissolved in 100 μL DMSO. After incubation for 10 min in a shaker, the absorption of the formazan is measured at 570 nm using a reader[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Male rats weighing 295 to 305 g are used. After a period of stabilization, 6 mg lipopolysaccharide/kg is administered intravenously in 0.3 mL over 2 min, and cardiovascular parameters are monitored over 5 to 6 h. L-Canavanine sulfate is administered intravenously in a 0.2 mL volume bolus injection at 100 mg/kg[1].

Mice: L-Canavanine is dissolved in phosphate-buffered saline[1]. L-Canavanine (100 mg/mb) is infused at a rate of 0.1 mL/hr through a catheter implanted S.C. over the back. Groups of 5 mice are treated at each dose beveltogether with 6 to 8 control animals and are inspected twice per day for median time of death[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Teale DM, et al. L-canavanine restores blood pressure in a rat model of endotoxic shock. Eur J Pharmacol. 1994 Dec 12;271(1):87-92.

    [2]. Nurcahyanti AD, et al. Cytotoxic potentiation of vinblastine and paclitaxel by L-canavanine in human cervical cancer and hepatocellular carcinoma cells. Phytomedicine. 2015 Dec 15;22(14):1232-7.

    [3]. Green MH, et al. Antitumor activity of L-canavanine against L1210 murine leukemia. Cancer Res. 1980 Mar;40(3):535-7.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Estrone sulfate potassium

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Estrone sulfate potassium  纯度: ≥99.0%

Estrone sulfate potassium 是一种天然的内源性类固醇,是雌激素酯和缀合物。

Estrone sulfate potassium

Estrone sulfate potassium Chemical Structure

CAS No. : 1240-04-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2750 In-stock
5 mg ¥2500 In-stock
10 mg ¥4000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Estrone sulfate potassium 相关产品

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生物活性

Estrone sulfate potassium is a natural endogenous steroid and is an estrogen ester and conjugate[1].

分子量

388.52

Formula

C18H21KO5S

CAS 号

1240-04-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL (321.73 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5739 mL 12.8694 mL 25.7387 mL
5 mM 0.5148 mL 2.5739 mL 5.1477 mL
10 mM 0.2574 mL 1.2869 mL 2.5739 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.43 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. O’Neil MM, et al. Differential Regulation of Gonadotropins in Response to Continuous Infusion of Native Gonadotropin-Releasing Hormone in the Winter Anovulatory Mare and Effects of Treatment With Estradiol-17β. J Equine Vet Sci. 2019 Apr;75:93-103.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Agmatine sulfate(Synonyms: 胍基丁胺;硫酸胍基丁胺;硫酸鲱精胺;胍基丁胺硫酸盐)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Agmatine sulfate (Synonyms: 胍基丁胺;硫酸胍基丁胺;硫酸鲱精胺;胍基丁胺硫酸盐) 纯度: ≥98.0%

Agmatine sulfate在多个靶点上发挥调节作用,如神经递质系统,离子通道,一氧化氮合成。它是 imidazoline receptor 的内源性激动剂和 NO synthase 抑制剂。

Agmatine sulfate(Synonyms: 胍基丁胺;硫酸胍基丁胺;硫酸鲱精胺;胍基丁胺硫酸盐)

Agmatine sulfate Chemical Structure

CAS No. : 2482-00-0

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in Water ¥500 In-stock
100 mg ¥450 In-stock
500 mg ¥800 In-stock
1 g ¥1100 In-stock
5 g   询价  
10 g   询价  

* Please select Quantity before adding items.

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生物活性

Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.

IC50 & Target

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Agmatine binds to alpha 2-adrenergic and imidazoline receptors and stimulates release of catecholamines from adrenal chromaffin cells. Its biosynthetic enzyme, arginine decarboxylase, is present in brain. Agmatine, locally synthesized, is an endogenous agonist at imidazoline receptors, a noncatecholamine ligand at alpha 2-adrenergic receptors and may act as a neurotransmitter[1]. Agmatine is synthesized in the brain, stored in synaptic vesicles in regionally selective neurons, accumulated by uptake, released by depolarization, and inactivated by agmatinase. Agmatine inhibits nitric oxide synthase, and induces the release of some peptide hormones[2]. Agmatine, 4-(aminobutyl)guanidine, is produced by decarboxylation of L-arginine by the enzyme arginine decarboxylase. Agmatine is a competitive inhibitor of all NOS isoenzymes but not an NO precursor. Ki values are approximately 660 µM (NOS I), 220 µM (NOS II) and 7.5 mM (NOS III)[3]. Agmatine stimulates nitrite production three-fold above basal nitrite formation by endothelial cells. Agmatine displaces [3H]-idazoxan from endothelial cellmembranes and is found to induce transients in the cytosolic calcium of endothelial cells. The transients could be downregulated by repeated exposure to agmatine but are not affected by pretreatment with norepinephrine[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Agmatine produces an antidepressant-like effect when assessed in the forced swimming test and in the tail suspension test in mice (dose range 0.01-50 mg/kg, i.p.), without accompanying changes in ambulation in an open-field[5]. In ischemic stroke, agmatine protects the blood-brain barrier, which can be monitored in vivo by quantification of permeability by using dynamic contrast-enhanced MR imaging[6]. Agmatine substantially augments the antidepressant-like effect of MK-801, reinforcing the notion that this compound modulates NMDA receptor activation[7].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

228.27

Formula

C5H16N4O4S

CAS 号

2482-00-0

中文名称

胍基丁胺;硫酸胍基丁胺;硫酸鲱精胺;胍基丁胺硫酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : ≥ 100 mg/mL (438.08 mM)

DMSO : 1 mg/mL (4.38 mM; ultrasonic and warming and heat to 80°C)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.3808 mL 21.9039 mL 43.8078 mL
5 mM 0.8762 mL 4.3808 mL 8.7616 mL
10 mM 0.4381 mL 2.1904 mL 4.3808 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Li G, et al. Agmatine: an endogenous clonidine-displacing substance in the brain. Science. 1994 Feb 18;263(5149):966-9.

    [2]. Reis DJ, et al. Is agmatine a novel neurotransmitter in brain? Trends Pharmacol Sci. 2000 May;21(5):187-93.

    [3]. Galea E, et al. Inhibition of mammalian nitric oxide synthases by agmatine, an endogenouspolyamine formed by decarboxylation of arginine. Biochem J. 1996 May 15;316 ( Pt 1):247-9.

    [4]. Morrissey JJ, et al. Agmatine activation of nitric oxide synthase in endothelial cells. Proc Assoc Am Physicians. 1997 Jan;109(1):51-7.

    [5]. Zomkowski AD, et al. Agmatine produces antidepressant-like effects in two models of depression in mice. Neuroreport. 2002 Mar 25;13(4):387-91.

    [6]. Ahn SS, et al. Effects of agmatine on blood-brain barrier stabilization assessed by permeability MRI in a rat model of transient cerebral ischemia. AJNR Am J Neuroradiol. 2015 Feb;36(2):283-8.

    [7]. Neis VB, et al. Agmatine enhances antidepressant potency of MK-801 and conventional antidepressants in mice. Pharmacol Biochem Behav. 2015 Mar;130:9-14.

Animal Administration
[6][7]

Rats: Thirty-four male Sprague-Dawley rats are subjected to transient MCA occlusion for 90 minutes. Immediately after reperfusion, agmatine (100 mg/kg) or normal saline is injected intraperitoneally into the agmatine-treated group (n= 17) or the control group, respectively. MR imaging is performed after reperfusion[6].

Mice: Mice are pretreated with a range of sub-effective doses of either fluoxetine (1, 2.5 and 5 mg/kg, p.o.; a selective serotonin reuptake inhibitor), imipramine (0.01, 0.05 and 0.1 mg/kg, p.o.; a tricyclic antidepressant), bupropion (0.1, 0.5 and 1 mg/kg, p.o.; dopamine reuptake inhibitor with subtle activity on noradrenergic reuptake), or MK-801 (0.0001, 0.0005 and 0.001 mg/kg, p.o.; noncompetitive NMDA receptor antagonist) and immediately after, a sub-effective dose of either agmatine (0.0001 mg/kg p.o.) or vehicle is administered. After 60 min, the animals are subjected to behavioral testing[7].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Li G, et al. Agmatine: an endogenous clonidine-displacing substance in the brain. Science. 1994 Feb 18;263(5149):966-9.

    [2]. Reis DJ, et al. Is agmatine a novel neurotransmitter in brain? Trends Pharmacol Sci. 2000 May;21(5):187-93.

    [3]. Galea E, et al. Inhibition of mammalian nitric oxide synthases by agmatine, an endogenouspolyamine formed by decarboxylation of arginine. Biochem J. 1996 May 15;316 ( Pt 1):247-9.

    [4]. Morrissey JJ, et al. Agmatine activation of nitric oxide synthase in endothelial cells. Proc Assoc Am Physicians. 1997 Jan;109(1):51-7.

    [5]. Zomkowski AD, et al. Agmatine produces antidepressant-like effects in two models of depression in mice. Neuroreport. 2002 Mar 25;13(4):387-91.

    [6]. Ahn SS, et al. Effects of agmatine on blood-brain barrier stabilization assessed by permeability MRI in a rat model of transient cerebral ischemia. AJNR Am J Neuroradiol. 2015 Feb;36(2):283-8.

    [7]. Neis VB, et al. Agmatine enhances antidepressant potency of MK-801 and conventional antidepressants in mice. Pharmacol Biochem Behav. 2015 Mar;130:9-14.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

B5培养基(不含琼脂和蔗糖)

上海金畔生物科技有限公司可以定制生产国产培养基,可以访问官网了解更多产品信息。
B5培养基(不含琼脂和蔗糖)

英文名称: B5 Medium
产品货号: JP8487-2
产品规格: 250g
90元
保质期: 三年
产品用途: 用于植物组织培养
备  注:

产品介绍:

用途:用于植物组织培养。

成分(mg/L):

Sodium Phosphate Monobasic/磷酸二氢钠

150

Calcium ChlorideAnhydrous/无水氯化钙

113.24

Potassium Nitrate/硝酸钾

2500

Ammonium Sulfate/硫酸铵

134

Magnesium Sulfate Anhydrous/无水硫酸镁

122.09

Na2EDTA/乙二胺四乙酸二钠

37.3

Ferrous Sulfate/硫酸亚铁

27.8

Manganese Sulfate/硫酸锰

10

Zinc Sulfate/硫酸锌

2

Boric Acid/硼酸

3

Sodium Molybdate/钼酸钠

0.25

Cupric Sulfate/硫酸铜

0.025

Cobalt Chloride.6H2O/氯化钴

0.025

Potassium lodide/碘化钾

0.75

Thiamine.HCI/盐酸硫胺素

10

Pyridoxine.HCI/盐酸吡哆醇

1

Nicotinic Acid/烟酸

1

Myo-Inositol/肌醇

100

pH值5.5

25℃

用法:
称取本品3.21g,加热溶解于1000ml 蒸馏水中,121℃高压灭菌15分钟,备用。

注:植物组织培养基,全无机盐配方,灭菌后有少量沉淀。


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250g 用于植物无土栽培营养液
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Atazanavir sulfate(Synonyms: 硫酸阿扎那韦; BMS-232632 sulfate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Atazanavir sulfate (Synonyms: 硫酸阿扎那韦; BMS-232632 sulfate) 纯度: 99.94%

Atazanavir sulfate (BMS-232632 sulfate) 是一种高选择性的 HIV-1蛋白酶抑制剂,用于艾滋病毒感染的研究。Atazanavir sulfate (BMS-232632 sulfate) 是 CYP3A4 的底物和抑制剂,也是 P-糖蛋白的抑制剂和诱导剂。Atazanavir sulfate 也是 SARS-CoV 3CLpro 的抑制剂,IC50 为 3.49 μM。

Atazanavir sulfate(Synonyms: 硫酸阿扎那韦; BMS-232632 sulfate)

Atazanavir sulfate Chemical Structure

CAS No. : 229975-97-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥770 In-stock
10 mg ¥700 In-stock
50 mg ¥2100 In-stock
100 mg ¥3100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].

IC50 & Target

HIV-1 protease[1]
CYP3A4, P-gp[2]

Clinical Trial

分子量

802.93

Formula

C38H54N6O11S

CAS 号

229975-97-7

中文名称

硫酸阿扎那韦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 166 mg/mL (206.74 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2454 mL 6.2272 mL 12.4544 mL
5 mM 0.2491 mL 1.2454 mL 2.4909 mL
10 mM 0.1245 mL 0.6227 mL 1.2454 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.11 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.11 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.11 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 4.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

  • 5.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Havlir DV, et al. Atazanavir: new option for treatment of HIV infection. Clin Infect Dis. 2004 Jun 1;38(11):1599-604.

    [2]. Wood R. Atazanavir: its role in HIV treatment. Expert Rev Anti Infect Ther. 2008 Dec;6(6):785-96.

    [3]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.

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Hydroxychloroquine-d4-1 sulfate(Synonyms: 羟氯喹 d4 (硫酸盐)(烷基上氘))

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Hydroxychloroquine-d4-1 sulfate (Synonyms: 羟氯喹 d4 (硫酸盐)(烷基上氘))

Hydroxychloroquine-d4-1 sulfate 是 Hydroxychloroquine 的氘代物。Hydroxychloroquine 是一种合成的抗疟疾剂,也可以抑制 Toll 样受体 7/9 (TLR7/9) 信号传导。Hydroxychloroquine 有效抑制 SARS-CoV-2 感染。

Hydroxychloroquine-d4-1 sulfate(Synonyms: 羟氯喹 d4 (硫酸盐)(烷基上氘))

Hydroxychloroquine-d4-1 sulfate Chemical Structure

CAS No. : 1216432-56-2

规格 是否有货
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10 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Hydroxychloroquine-d4-1 sulfate is the deuterium labeled Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

437.97

Formula

C18H24D4ClN3O5S

CAS 号

1216432-56-2

中文名称

羟氯喹 d4 (硫酸盐)(烷基上氘)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Manzo C, et al. Psychomotor Agitation Following Treatment with Hydroxychloroquine. Drug Saf Case Rep. 2017 Dec;4(1):6.

    [3]. Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol. 2014 Mar;85(3):429-40.

    [4]. Yao X, et al. In Vitro Antiviral Activity and Projection of Optimized Dosing Design of Hydroxychloroquine for the Treatment of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). Clin Infect Dis. 2020 Mar 9. pii: ciaa237.

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Iobenguane sulfate(Synonyms: MIBG sulfate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Iobenguane sulfate (Synonyms: MIBG sulfate) 纯度: 99.94%

Iobenguane sulfate (MIBG sulfate) 是一种具有抗肿瘤活性的神经递质去甲肾上腺素的类似物。放射性碘代 Iobenguane sulfate 可用于肾上腺肿瘤诊断和肿瘤靶向药物的研究。Iobenguane sulfate 是一种高亲和力的霍乱毒素底物,干扰细胞单核(ADP-核糖基化)。

Iobenguane sulfate(Synonyms: MIBG sulfate)

Iobenguane sulfate Chemical Structure

CAS No. : 87862-25-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥880 In-stock
5 mg ¥800 In-stock
10 mg ¥1150 In-stock
25 mg ¥2650 In-stock
50 mg ¥4750 In-stock
100 mg ¥8650 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Iobenguane sulfate 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Anti-Blood Cancer Compound Library

生物活性

Iobenguane sulfate (MIBG sulfate) is an analogue of the neurotransmitter norepinephrine with antitumor activity. Radioiodinated Iobenguane sulfate is clinically used as a tumor-targeted radiopharmaceutical in the diagnosis and treatment of adrenergic tumors. Iobenguane sulfate is a high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation)[1][2].

体外研究
(In Vitro)

Iobenguane sulfate (MIBG sulfate) (2-20 μg/ml; 72 hours) inhibits cell growth in a panel of human and mouse leukemia, fibrosarcoma, melanoma, and neuroblastoma cell lines[1].
Iobenguane sulfate (MIBG sulfate) is a potent affector of endogenous mono(ADP-ribosyl) transferases of turkey and human erythrocyte membranes, exerting its effect in the μM concentration range[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: 3T3, 3T3-Tl3, BHK, Py-BHK, K562, L1210, RIF1, M5A, B16, LAN-1, N1E115, CHP212 cells
Concentration: 2, 20μg/ml
Incubation Time: 72 hours
Result: Inhibits 3T3, 3T3-Tl3, BHK, Py-BHK, K562, L1210, RIF1, M5A, B16, LAN-1, N1E115, and CHP212 cells growth.

体内研究
(In Vivo)

Iobenguane sulfate (MIBG hemisulfate) (20 mg/kg; i.p.; daily on days 3-6) shows antitumor activity[1].
The survival of male strain AF mice inoculates with N1E115 neuroblastoma and treats according to NIH protocols for new drug testing with 9 daily injections of Iobenguane sulfate (40 mg/kg), Marking prolongation of sugvival but no cures were observed[1].
Iobenguane sulfate testes for its toxicity on male strain AF (N1Ell5) mice with 5 daily injections. At 50 mg/kg body weight, all animals died after 1-4 doses and 4/16 animals died on a schedule of 44 mg/kg[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: DBA/2 (L1210)) mice[1]
Dosage: i.p.; daily on days 3-6
Administration: 20 mg/kg
Result: Considerable prolongation of survival and some cures were obtained.

分子量

324.13

Formula

C8H12IN3O4S

CAS 号

87862-25-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (308.52 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0852 mL 15.4259 mL 30.8518 mL
5 mM 0.6170 mL 3.0852 mL 6.1704 mL
10 mM 0.3085 mL 1.5426 mL 3.0852 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.71 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.71 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.71 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Loesberg C, et al. Meta-iodobenzylguanidine (MIBG), a novel high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation). Biochim Biophys Acta. 1990 Jan 19;1037(1):92-9.

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Vincristine-d3 sulfate(Synonyms: Leurocristine-d3 sulfate; NSC-67574-d3 sulfate; 22-Oxovincaleukoblastine-d3 sulfate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Vincristine-d3 sulfate (Synonyms: Leurocristine-d3 sulfate; NSC-67574-d3 sulfate; 22-Oxovincaleukoblastine-d3 sulfate)

Vincristine-d3 (Leurocristine-d3) sulfate 是 Vincristine sulfate 的氘代物。Vincristine sulfate是一种抗肿瘤长春花生物碱,抑制有丝分裂纺锤体中的 microtubule 形成,导致中期阶段的分裂细胞停滞。 它与 microtubule 结合的 Ki 为85 nM。

Vincristine-d3 sulfate(Synonyms: Leurocristine-d3 sulfate; NSC-67574-d3 sulfate; 22-Oxovincaleukoblastine-d3 sulfate)

Vincristine-d3 sulfate Chemical Structure

CAS No. : 1246817-10-6

规格 是否有货
1 mg Check price and availability
10 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Vincristine-d3 (Leurocristine-d3) sulfate is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

926.05

Formula

C46H55D3N4O14S

CAS 号

1246817-10-6

中文名称

硫酸长春新碱 d3 (硫酸盐)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Jordan, M.A., et al. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro. Cancer Res, 1985. 45(6): p. 2741-7.

    [3]. Gidding, C.E., et al, Vincristine revisited. Crit Rev Oncol Hematol, 1999. 29(3): p. 267-87.

    [4]. Donoso, J.A., et al, Action of the vinca alkaloids vincristine, vinblastine, and desacetyl vinblastine amide on axonal fibrillar organelles in vitro. Cancer Res, 1977. 37(5): p. 1401-7.

    [5]. Horton, J.K., et al. Relationships between tumor responsiveness, vincristine pharmacokinetics and arrest of mitosis in human tumor xenografts. Biochem Pharmacol, 1988. 37(20): p. 3995-4000.

    [6]. Baguley, B.C., et al, Inhibition of growth of colon 38 adenocarcinoma by vinblastine and colchicine: evidence for a vascular mechanism. Eur J Cancer, 1991. 27(4): p. 482-7.

    [7]. Zhang D, et al. Co-delivery nanoparticles with characteristics of intracellular precision release drugs for overcoming multidrug resistance. Int J Nanomedicine. 2017 Mar 16;12:2081-2108.

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Hydroxychloroquine-d4 sulfate(Synonyms: HCQ-d4 sulfate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Hydroxychloroquine-d4 sulfate (Synonyms: HCQ-d4 sulfate)

Hydroxychloroquine-d4 sulfate (HCQ-d4 sulfate) 是 Hydroxychloroquine sulfate 的氘代物。Hydroxychloroquine (HCQ) sulfate 是一种合成的抗疟疾剂,也可以抑制 Toll 样受体 7/9 (TLR7/9) 信号传导。Hydroxychloroquine sulfate 有效抑制 SARS-CoV-2 感染。

Hydroxychloroquine-d4 sulfate(Synonyms: HCQ-d4 sulfate)

Hydroxychloroquine-d4 sulfate Chemical Structure

CAS No. : 1854126-45-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Hydroxychloroquine-d4 sulfate (HCQ-d4 sulfate) is the deuterium labeled Hydroxychloroquine sulfate. Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

437.97

Formula

C18H24D4ClN3O5S

CAS 号

1854126-45-6

中文名称

硫酸羟氯喹 d4 (硫酸盐)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Manzo C, et al. Psychomotor Agitation Following Treatment with Hydroxychloroquine. Drug Saf Case Rep. 2017 Dec;4(1):6.

    [3]. Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol. 2014 Mar;85(3):429-40.

    [4]. Yao X, et al. In Vitro Antiviral Activity and Projection of Optimized Dosing Design of Hydroxychloroquine for the Treatment of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). Clin Infect Dis. 2020 Mar 9. pii: ciaa237.

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Coptisine Sulfate(Synonyms: 硫酸黄连碱)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Coptisine Sulfate (Synonyms: 硫酸黄连碱)

Coptisine Sulfate 是从黄连中分离到的生物碱,是一种有效的非竞争性的 IDO 抑制剂,Ki 值为 5.8 μM,IC50 值为 6.3 μM。

Coptisine Sulfate(Synonyms: 硫酸黄连碱)

Coptisine Sulfate Chemical Structure

CAS No. : 1198398-71-8

规格 价格 是否有货
5 mg ¥800 询问价格 & 货期
10 mg ¥1350 询问价格 & 货期
25 mg ¥2450 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Coptisine Sulfate is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM[1].

IC50 & Target

IC50: 6.3 μM (IDO)[1]
Ki: 5.8 μM (IDO)[1]

分子量

417.39

Formula

C19H15NO8S

CAS 号

1198398-71-8

中文名称

黄连碱硫酸盐;硫酸黄连碱

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Yu D, et al. The IDO inhibitor coptisine ameliorates cognitive impairment in a mouse model of Alzheimer’s disease. J Alzheimers Dis. 2015;43(1):291-302.

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Demethylwedelolactone Sulfate(Synonyms: Demethylwedelolactone 3-sulfate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Demethylwedelolactone Sulfate (Synonyms: Demethylwedelolactone 3-sulfate)

Demethylwedelolactone Sulfate (Demethylwedelolactone 3-sulfate) 是从 Eclipta prostrata L. 分离出的一种香豆素类化合物。

Demethylwedelolactone Sulfate(Synonyms: Demethylwedelolactone 3-sulfate)

Demethylwedelolactone Sulfate Chemical Structure

CAS No. : 1318240-80-0

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生物活性

Demethylwedelolactone Sulfate (Demethylwedelolactone 3-sulfate) is a coumestan isolated from Eclipta prostrata L.[1].

分子量

380.28

Formula

C15H8O10S

CAS 号

1318240-80-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Chao-Feng Zhang, et al. Sulphur compounds from the aerial parts of Eclipta prostrata. Biochemical Systematics and Ecology. (2010);38(6):1253–1256.

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Momelotinib sulfate(Synonyms: CYT387 sulfate salt)

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Momelotinib sulfate (Synonyms: CYT387 sulfate salt) 纯度: 98.04%

Momelotinib sulfate (CYT387 sulfate salt) 是一种 ATP竞争性的 JAK1/JAK2 抑制剂,IC50 分别为 11 nM/18 nM,作用于JAK3时,IC50 为 155 nM。

Momelotinib sulfate(Synonyms: CYT387 sulfate salt)

Momelotinib sulfate Chemical Structure

CAS No. : 1056636-06-6

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生物活性

Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).

IC50 & Target[1]

JAK1

11 nM (IC50)

JAK2

18 nM (IC50)

JAK3

155 nM (IC50)

体外研究
(In Vitro)

Momelotinib sulfate (CYT387 sulfate salt) inhibits growth of Ba/F3-JAK2V617F and human erythroleukemia (HEL) cells (IC50=1.5 μM) or Ba/F3-MPLW515L cells (IC50=200 nM), but has considerably less activity against BCR-ABL harboring K562 cells (IC50=58 μM) and FLT3 mutation harboring MV4-11 cells (IC50=3 μM). Proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated with IL-3 is inhibited with an IC50 value of 1.4 μM, consistent with the established role of IL-3-dependent signaling in the parental cell line[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Momelotinib sulfate (CYT387 sulfate salt) at twice the dose used in disease model (50 and 100 mg/kg) has little to no effect on peripheral blood counts over a period of 8 weeks. Median plasma peak concentrations are 7.1 μM with the lower dose and 32.1μM with the higher dose, with a half-life of approximately 2 hours. Trough levels at 12 hours are 10nM for the 25 mg/kg and 900nM for the 50 mg/kg dose. At day 34 after transplantation, the mean white blood cell counts and hematocrit values of the entire cohort exceeded the normal range for Balb/c mice by more than 1 SD. At this point, 6 mice are sacrificed and subjected to autopsy. In the remaining animals, treatment is initiated with 25 mg/kg Momelotinib sulfate (CYT387 sulfate salt), 50 mg/kg Momelotinib sulfate (CYT387 sulfate salt), or vehicle, administered twice daily by oral gavage (12 mice per treatment group). A rapid drop of the white cell counts is apparent in both dose cohorts as early as 6 days after initiation of treatment and a decline of the hematocrit is apparent after 20 days[2]. After oral dosing, Momelotinib sulfate (CYT387 sulfate salt) exhibits high plasma concentrations (Cmax= 40.4 μM; Tmax=4 h), with quantitative absolute oral bioavailability and an apparent half life of 2.4 h. The high oral bioavailability, can likely be partly ascribed to the low blood clearance of Momelotinib sulfate (CYT387 sulfate salt) (6.3 mL/min/kg) and therefore low susceptibility to hepatic first pass metabolism[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

610.62

Formula

C23H26N6O10S2

CAS 号

1056636-06-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 220 mg/mL (360.29 mM; Need ultrasonic)

H2O : 100 mg/mL (163.77 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6377 mL 8.1884 mL 16.3768 mL
5 mM 0.3275 mL 1.6377 mL 3.2754 mL
10 mM 0.1638 mL 0.8188 mL 1.6377 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5.5 mg/mL (9.01 mM); Clear solution

    此方案可获得 ≥ 5.5 mg/mL (9.01 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5.5 mg/mL (9.01 mM); Clear solution

    此方案可获得 ≥ 5.5 mg/mL (9.01 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 5.5 mg/mL (9.01 mM); Clear solution

    此方案可获得 ≥ 5.5 mg/mL (9.01 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445.

    [2]. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240.

    [3]. Burns CJ, et al. Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92.

Kinase Assay
[1]

Glutathione-S-transferase (GST)-tagged JAK kinase domains expressed in insect cells are purified before use in a peptide substrate phosphorylation assay. Assays are carried out in 384-well optiplates using an Alphascreen Protein Tyrosine Kinase P100 detection kit and a PerkinElmer Fusion Alpha instrument[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Ba/F3 cells expressing JAK2V617F (Ba/F3-JAK2V617F) and MPLW515L (Ba/F3-MPLW515L) mutants, as well as CHRF-288-11 (JAK2T875N) and CMK (JAK3A572V) cells are used. The TEL/JAK2 and TEL/JAK3 fusions are generated and introduced into Ba/F3 murine cells. TheTEL/JAK2– or TEL/JAK3-transfected cells are cultured in Dulbecco’s modified Eagle’s medium (DMEM) containing 10% fetal calf serum (FCS). Ba/F3 wild-type cells are cultured in RPMI containing 10% FCS supplemented with 5 ng/mL murine IL-3. Proliferation is measured using the Alamar Blue assay after incubating for 72 h at 37°C with 5% CO2[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]

On day 32 after bone marrow transplantation (when all mice exhibit severe leukocytosis and erythrocytosis), mice are assigned to 3 groups such that each group has equivalent average body weight and blood counts. Momelotinib (CYT387) is dissolved in NMP (120 mg/mL final; 1-methyl-2-pyrrolidinone, Chromasolv Plus). Subsequently, the Momelotinib/NMP mix is diluted with 0.14M Captisol to a concentration of 6 mg/mL and further diluted with 0.1M Captisol to a final concentration of 4 mg/mL. All 3 groups of mice (n=12 per group) are administered Momelotinib (CYT387) by oral gavage twice daily at 10- to 12-hour intervals from day 34 after bone marrow transplantation to day 82 (end of experiment). Mice receive NMP/Captisol without Momelotinib (CYT387) (0 mg/kg group), 25 mg/kg Momelotinib, or 50 mg/kg Momelotinib. At day 82 after bone marrow transplantation, all mice are euthanized for analysis except for 2 mice each from the 50 mg/kg and 25 mg/kg groups, which are taken off Momelotinib (CYT387) treatment and followed for 45 additional days. For assessment of the effects of Momelotinib (CYT387) on normal blood counts, naive Balb/c mice are administered vehicle control, 50 mg/kg, or 100 mg/kg Momelotinib (CYT387) in an identical fashion as described for the bone marrow transplant experimental mouse cohort. Peripheral blood is drawn at day 14, 28, 42, and 56 and levels of red cells, white cells, reticulocytes, granulocytes, lymphocytes, and monocytes are analyzed.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445.

    [2]. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240.

    [3]. Burns CJ, et al. Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92.

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Quinidine sulfate dihydrate(Synonyms: 硫酸奎尼宁)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Quinidine sulfate dihydrate (Synonyms: 硫酸奎尼宁)

Quinidine sulfate dihydrate 是一种抗心律失常剂,也是 K+ 通道 (K+ channel) 的有效阻断剂,其 IC50 值为 19.9 μM。Quinidine sulfate dihydrate 是一种有效且选择性的细胞色素 P450db (cytochrome P450db) 抑制剂,也可用作疟疾的研究。

Quinidine sulfate dihydrate(Synonyms: 硫酸奎尼宁)

Quinidine sulfate dihydrate Chemical Structure

CAS No. : 6591-63-5

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5 mg 询价
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生物活性

Quinidine sulfate dihydrate is a potent and selective inhibitor of cytochrome P450db and inhibits amphetamine metabolism in vivo[1]. Quinidine sulfate dihydrate enhances the cytotoxicity of vincristine (VCR) in tumor cells and especially in VCR-resistant sublines of P388 leukemia (P388/VCR) and human myelogenous leukemia[2].

IC50 & Target

IC50: cytochrome P450db; amphetamine metabolism[1]

Clinical Trial

分子量

405.50

Formula

C21H30N2O7S

CAS 号

6591-63-5

中文名称

硫酸奎尼宁

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. David E. Moody, et al. Quinidine Inhibits In Vivo Metabolism of Amphetamine in Rats: Impact upon Correlation between GCIMS and Immunoassay Findings in Rat Urine. ournal of Analytical Toxicology, Vol. 14, September/October 1990

    [2]. Tsuruo T, et al. Effects of quinidine and related compounds on cytotoxicity and cellular accumulation of vincristine and adriamycin in drug-resistant tumor cells.Cancer Res. 1984 Oct;44(10):4303-7.

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Glucosamine sulfate(Synonyms: 硫酸氨基葡萄糖; D-Glucosamine sulfate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Glucosamine sulfate (Synonyms: 硫酸氨基葡萄糖; D-Glucosamine sulfate) 纯度: ≥98.0%

Glucosamine sulfate (D-Glucosamine sulfate) 是一种氨基糖, 是糖基化蛋白和脂质生化合成的突出前体, 用作膳食补充剂。Glucosamine sulfate 也是软骨基质和滑液中糖胺聚糖的天然成分,当外用时,对骨关节炎软骨和软骨细胞具有药理作用。

Glucosamine sulfate(Synonyms: 硫酸氨基葡萄糖; D-Glucosamine sulfate)

Glucosamine sulfate Chemical Structure

CAS No. : 29031-19-4

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生物活性

Glucosamine sulfate (D-Glucosamine sulfate) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine sulfate also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes[1].

IC50 & Target[1]

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Glucosamine sulfate (D-Glucosamine sulfate) exhibits dose-dependent DPPH antioxidant activity[2].
Glucosamine sulfate treatment of Short-term (4 h) inhibits HIF-1α at the protein level, decreases phosphorylation of p70S6K and S6, translation-related proteins[3].
Glucosamine sulfate significantly decreases renal expression of α-smooth muscle actin, collagen I, and fibronectin in the obstructed kidneys and TGF-β1-treated renal cells[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

277.25

Formula

C6H15NO9S

CAS 号

29031-19-4

中文名称

硫酸氨基葡萄糖;氨基葡萄糖硫酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 125 mg/mL (450.86 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6069 mL 18.0343 mL 36.0685 mL
5 mM 0.7214 mL 3.6069 mL 7.2137 mL
10 mM 0.3607 mL 1.8034 mL 3.6069 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Bruyère O, et al. Efficacy and safety of glucosamine sulfate in the management of osteoarthritis: Evidence from real-life setting trials and surveys. Semin Arthritis Rheum. 2016 Feb;45(4 Suppl):S12-7.

    [2]. Jamialahmadi K, et al. Protective effects of glucosamine hydrochloride against free radical-induced erythrocytes damage. Environ Toxicol Pharmacol. 2014 Jul;38(1):212-9.

    [3]. Jo JR, et al. Short-term treatment with glucosamine hydrochloride specifically downregulates hypoxia-inducible factor-1α at the protein level in YD-8 human tongue cancer cells. Int J Oncol. 2014 May;44(5):1699-706.

    [4]. Park J, et al. Glucosamine hydrochloride exerts a protective effect against unilateral ureteral obstruction-induced renal fibrosis by attenuating TGF-β signaling. J Mol Med (Berl). 2013 Nov;91(11):1273-84.

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NVP-CGM097 sulfate(Synonyms: CGM097 sulfate)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

NVP-CGM097 sulfate (Synonyms: CGM097 sulfate) 纯度: 98.76%

NVP-CGM097是有效,选择性的MDM2抑制剂;IC50值为1.7 nM。

NVP-CGM097 sulfate(Synonyms: CGM097 sulfate)

NVP-CGM097 sulfate Chemical Structure

CAS No. : 1313367-56-4

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生物活性

NVP-CGM097 sulfate is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.

IC50 & Target

IC50 & Target: IC50: 1.7±0.1 nM (hMDM2)[1]

体外研究
(In Vitro)

NVP-CGM097 binds to human MDM2 with an IC50 of 1.7 nM and shows high selectivity over MDM4 (IC50=2000 nM). NVP-CGM097 is about four times more potent than Nutlin-3a (IC50=8 nM). In addition, NVP-CGM097 shows no significant activity against Bcl-2:Bak, Bcl-2:Bad, Mcl-1:Bak, Mcl-1:NOXA, XIAP:BIR3, and c-IAP:BIR3 protein-protein interactions. NVP-CGM097 significantly inhibits the proliferation of cells expressing wild-type p53, while sparing the p53 null cells with a 35-58-fold difference. NVP-CGM097 is able to significantly redistribute wild-type p53 into the cell nucleus with an IC50 of 0.224 μM, demonstrating its ability to inhibit the p53:MDM2 interaction in living cells. NVP-CGM097 significantly inhibits the proliferation of cells expressing wild-type p53, while sparing the p53 null cells with a 35-58-fold difference. NVP-CGM097 inhibtis HCT116 (p53WT/WT) with IC50 of 454±136 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NVP-CGM097 is able to inhibit the interaction between p53 and MDM2 and reactivate the p53 pathway in a MDM2-amplified SJSA-1 human tumor model, as judged by elevation of p21 mRNA levels, a pharmacodynamic (PD) indicator for p53 activity. p21 mRNA levels are found to increase concomitantly with levels of NVP-CGM097 in tumor-bearing rats dosed at 30 mg/kg. The PD response is biphasic and prolonged up to 24 h. Additional p53 target genes such as MDM2 and PUMA mRNA levels are assessed in the tumor samples as well and showed a similar behavior. Daily treatment with NVP-CGM097 dose dependently and significantly inhibits SJSA-1 tumor growth in rats. It promotes stable disease at 20 mg/kg, which is associated with a plasma AUC0-24 of 163 μM•h. After iv administration, the total blood clearance (CL) of NVP-CGM097 is 5 mL/min per kg for mouse, 7 mL/min per kg for rat, 3 mL/min per kg for dog, and 4 mL/min per kg for monkey. The apparent terminal half-life (t1/2) is long in rodents and monkey (6-12 h) but is comparatively longer in dogs (20 h). After oral dosing, NVP-CGM097 is well absorbed with Tmax occurring between 1 and 4.5 h in all species tested[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

757.34

Formula

C38H49ClN4O8S

CAS 号

1313367-56-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (132.04 mM; Need ultrasonic)

H2O : 100 mg/mL (132.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3204 mL 6.6021 mL 13.2041 mL
5 mM 0.2641 mL 1.3204 mL 2.6408 mL
10 mM 0.1320 mL 0.6602 mL 1.3204 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.30 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.30 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.30 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.30 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.30 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.30 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Holzer P, et al. Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. J Med Chem. 2015 Aug 27;58(16):6348-58.

Cell Assay
[1]

Two pairs of cell lines are used to assess NVP-CGM097 p53-dependent antiproliferative effects: (1) an isogenic pair of HCT116 cell lines either expressing wild-type p53 or knocked-out for the p53 gene and (2) a nonisogenic pair of osteosarcoma cell lines either endogenously expressing wild-type p53 and amplified for MDM2 (SJSA-1 cells) or null for p53 (SAOS-2 cells)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Female athymic rats bearing subcutaneous xenotransplants of SJSA-1 tumors (n=5-12) are treated at 5, 10, 20, or 30 mg/kg or three times a week on Monday, Wednesday, and Friday (3qw M, W, F) at 30 or 70 mg/kg po for 14 days. Plasma AUCs are determined at the end of the study. Positive numbers indicate the percentage of tumor growth inhibition (T/C); negative numbers indicate the percentage of tumor regression[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Holzer P, et al. Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. J Med Chem. 2015 Aug 27;58(16):6348-58.

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