Dihydroactinidiolide(Synonyms: 二氢猕猴桃内酯)

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。

Dihydroactinidiolide (Synonyms: 二氢猕猴桃内酯)

Dihydroactinidiolide 存在于植物叶片和果实中,是有效的植物生长抑制剂,基因表达的调节剂,同时负责拟南芥中的光适应。Dihydroactinidiolide 具有抗氧化活性,抗菌活性,抗癌活性和神经保护作用。

Dihydroactinidiolide(Synonyms: 二氢猕猴桃内酯)

Dihydroactinidiolide Chemical Structure

CAS No. : 17092-92-1

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生物活性

Dihydroactinidiolide, existing in plant leaves and fruits, is a potent plant growth inhibitor, a regulator of gene expression and is responsible for photo acclimation in Arabidopsis. Dihydroactinidiolide has antioxidant activity, antibacterial activity, anticancer activity and neuroprotective effect[1].

分子量

180.24

Formula

C11H16O2

CAS 号

17092-92-1

中文名称

二氢猕猴桃内酯

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]. Das M, et al. Dihydroactinidiolide, a natural product against Aβ25-35 induced toxicity in Neuro2a cells: Synthesis, in silico and in vitro studies. Bioorg Chem. 2018 Dec;81:340-349.

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(E/Z)-E64FC26

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。

(E/Z)-E64FC26  纯度: 99.44%

(E/Z)-E64FC26 是 E-E64FC26 和 Z-E64FC26 的混合物。E64FC26 (E-E64FC26) 是蛋白质二硫键异构酶 (PDI) 家族的一种有效的泛抑制剂,对 PDIA1、PDIA3、PDIA4、TXNDC5 和 PDIA6 的 IC50 分别为 1.9、20.9、25.9、16.3 和 25.4 μM。E64FC26 显示抗骨髓瘤活性。

(E/Z)-E64FC26

(E/Z)-E64FC26 Chemical Structure

CAS No. : 2285446-67-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3850 In-stock
5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
50 mg ¥16500 In-stock
100 mg ¥25500 In-stock
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生物活性

(E/Z)-E64FC26 is a mixture complex of E-E64FC26 and Z-E64FC26. E64FC26 (E-E64FC26) is a potent pan-inhibitor of the protein disulfide isomerase (PDI) family, with IC50s of 1.9, 20.9, 25.9, 16.3, and 25.4 μM against PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6. E64FC26 shows anti-myeloma activity[1][2].

分子量

340.38

Formula

C19H23F3O2

CAS 号

2285446-67-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (293.79 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9379 mL 14.6895 mL 29.3789 mL
5 mM 0.5876 mL 2.9379 mL 5.8758 mL
10 mM 0.2938 mL 1.4689 mL 2.9379 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。-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    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (7.34 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.34 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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
*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]. Nathan G. Dolloff, et al. Indene derivatives and uses thereof. US20190062298A1.

    [2]. Robinson RM, et al. Inhibitors of the protein disulfide isomerase family for the treatment of multiple myeloma. Leukemia. 2019 Apr;33(4):1011-1022.

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Pironetin

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。

Pironetin 

Pironetin 是从链霉菌属物种分离的 α/β 不饱和内酯。Pironetin 与 α-tubulin 结合,是微管聚合的有效抑制剂,具有细胞周期停滞和抗肿瘤活性。

Pironetin

Pironetin Chemical Structure

CAS No. : 151519-02-7

规格 价格 是否有货
1 mg ¥28000 询问价格 & 货期

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生物活性

Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity[1][2].

IC50 & Target

Microtubule[1]

体外研究
(In Vitro)

Pironetin (20-100 ng/mL; 24 hours; 3Y1 cells) treatment arrests the cell cycle progression at G2/M in 3Y1 cells[1].
Pironetin (1-10000 ng/mL; 3 days; HeLa, A2780 and K-NRK cells) treatment inhibits the cell proliferation. IC50 values against these cell lines are almost 10 ng/mL[1].

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

Cell Cycle Analysis[1]

Cell Line: 3Y1 cells
Concentration: 20 ng/mL, 50 ng/mL, 100 ng/mL
Incubation Time: 24 hours
Result: Arrested the cell cycle progression at G2/M in3Y1 cells.

Cell Proliferation Assay[1]

Cell Line: HeLa, A2780 and K-NRK cells
Concentration: 1 ng/mL, 10 ng/mL, 100 ng/mL, 1000 ng/mL and 10000 ng/mL
Incubation Time: 3 days
Result: Inhibited the cell proliferation.

体内研究
(In Vivo)

Pironetin (0.78-6.25 mg/kg; intraperitoneal injection; daily; for 5 days; female CDF1-SLC mice) treatment shows a moderate antitumor effect, however, a severe weight loss is observed as a side effect[1].

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

Animal Model: Female CDF1-SLC mice (10 weeks) injected with P388 murine leukemia cells[1]
Dosage: 0.78 mg/kg, 1.56 mg/kg, 3.13 mg/kg, 6.25 mg/kg
Administration: Intraperitoneal injection; daily; for 5 days
Result: Showed a moderate antitumor effect.

分子量

324.45

Formula

C19H32O4

CAS 号

151519-02-7

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]. Kondoh M, et al. Cell cycle arrest and antitumor activity of pironetin and its derivatives. Cancer Lett. 1998 Apr 10;126(1):29-32.

    [2]. Yang J, et al. Pironetin reacts covalently with cysteine-316 of α-tubulin to destabilize microtubule. ] Nat Commun. 2016 Jun 30;7:12103.

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Methyl gallate(Synonyms: Gallincin; NSC 363001)

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。

Methyl gallate (Synonyms: Gallincin; NSC 363001) 纯度: 99.96%

Methyl gallate是具有抗氧化,抗癌和抗炎活性的植物酚类。Methyl gallate也可抑制细菌活性。Methyl gallate 还具有抗 HIV-1HIV-1 酶的抑制活性。

Methyl gallate(Synonyms: Gallincin;  NSC 363001)

Methyl gallate Chemical Structure

CAS No. : 99-24-1

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥500 In-stock
500 mg ¥400 In-stock
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生物活性

Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitory activities.

IC50 & Target

Bacterial[1]

体外研究
(In Vitro)

The growth of A. viscosus is inhibited completely by a low dose of Methyl gallate (MIC=1 mg/mL). S. mutans and . sobrinus show intermediate sensitivity to Methyl gallate (MIC=2-4 mg/mL), whereas the growth of Lactobacillus spp. is inhibited completely at a relatively high concentration (MIC=8 mg/mL)[1]. Methyl gallate, in a concentration of 100 mM, could alleviate lipid peroxidation of the cells exposed to a short-term H2O2 treatment. In addition, Methyl gallate-treated cells could prevent intracellular glutathione (GSH) from being depleted following an exposure of H2O2 (8.0 mM) for a 3 h period[2]. Methyl gallate inhibits Treg cell-suppressive effects on effector CD4+ T cells and Treg migration toward tumor environment. Furthermore, forkhead box P3 (Foxp3) expression is also significantly decreased by methyl gallate[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

184.15

Formula

C8H8O5

CAS 号

99-24-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (543.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.4304 mL 27.1518 mL 54.3036 mL
5 mM 1.0861 mL 5.4304 mL 10.8607 mL
10 mM 0.5430 mL 2.7152 mL 5.4304 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。-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 (13.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (13.58 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 (13.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (13.58 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 (13.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (13.58 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]. Kang MS, et al. Inhibitory effect of methyl gallate and gallic acid on oral bacteria. J Microbiol. 2008 Dec;46(6):744-50.

    [2]. Hsieh TJ, et al. Protective effect of methyl gallate from Toona sinensis (Meliaceae) against hydrogen peroxide-induced oxidative stress and DNA damage in MDCK cells. Food Chem Toxicol. 2004 May;42(5):843-50.

    [3]. Lee H, et al. Methyl gallate exhibits potent antitumor activities by inhibiting tumor infiltration of CD4+CD25+ regulatory T cells. J Immunol. 2010 Dec 1;185(11):6698-705.

    [4]. Wang CR, et al. First report on isolation of methyl gallate with antioxidant, anti-HIV-1 and HIV-1 enzyme inhibitory activities from a mushroom (Pholiota adiposa). Environ Toxicol Pharmacol. 2014 Mar;37(2):626-37.

Cell Assay
[1]

KB cells, a human mouth epithelial cell line, are treated with Methyl gallate (1-8 mg/mL) for 24 h. Cytotoxicity of Methyl gallate is assessed by a modified MTT assay[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]. Kang MS, et al. Inhibitory effect of methyl gallate and gallic acid on oral bacteria. J Microbiol. 2008 Dec;46(6):744-50.

    [2]. Hsieh TJ, et al. Protective effect of methyl gallate from Toona sinensis (Meliaceae) against hydrogen peroxide-induced oxidative stress and DNA damage in MDCK cells. Food Chem Toxicol. 2004 May;42(5):843-50.

    [3]. Lee H, et al. Methyl gallate exhibits potent antitumor activities by inhibiting tumor infiltration of CD4+CD25+ regulatory T cells. J Immunol. 2010 Dec 1;185(11):6698-705.

    [4]. Wang CR, et al. First report on isolation of methyl gallate with antioxidant, anti-HIV-1 and HIV-1 enzyme inhibitory activities from a mushroom (Pholiota adiposa). Environ Toxicol Pharmacol. 2014 Mar;37(2):626-37.

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Pinosylvin

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。

Pinosylvin  纯度: 99.66%

Pinosylvin 是从 Pinus spp 的心材中分离出来的一种感染前的类苯乙烯类毒素,具有抗菌 (anti-bacterial) 活性。 Pinosylvin 是一种白藜芦醇的类似物,可以诱导白血病细胞凋亡 (apoptosis) 和自噬 (autophapy)。

Pinosylvin

Pinosylvin Chemical Structure

CAS No. : 22139-77-1

规格 价格 是否有货 数量
5 mg ¥3360 In-stock
10 mg ¥5710 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

Pinosylvin is a pre-infectious stilbenoid toxin isolated from the heartwood of Pinus spp, has anti-bacterial activities[1]. Pinosylvin is a resveratrol analogue, can induce cell apoptosis and autophapy in leukemia cells[2].

体外研究
(In Vitro)

Pinosylvin (0-100 μM; 24 hours) is cytotoxic to THP‐1 and U937 cells, exhibits an IC50 value of 20-30 μM in leukemia cells, the maximal cytotoxic effect occurred at 100 μM following incubation for 24 hr[3].
Pinosylvin (0-100 μM; 24 hours) enhances the number of annexin V+ and PI+ cells in the U937 population at 50 μM, increases annexin V+ and PI+ cells in the THP‐1 population at 100 μM[3].
Pinosylvin (0-100 μM; 24 hours) promotes autophagy in leukemia cells by enhancing the level of LC3‐II and p62/SQSTM1 degradation in leukemia cells[3].

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

Cell Viability Assay[3]

Cell Line: Leukemia cells
Concentration: 0 μM; 0.1 μM; 1 μM; 10 μM; 50 μM; 100 μM
Incubation Time: 24 hours
Result: Was cytotoxic to leukemia cells at high concentrations.

Apoptosis Analysis[3]

Cell Line: U937 and THP‐1 cells
Concentration: 0 μM; 0.1 μM; 1 μM; 10 μM; 50 μM; 100 μM
Incubation Time: 24 hours
Result: Induced apoptosis cell number in U937 and THP‐1 cells.

Western Blot Analysis[3]

Cell Line: U937 and THP‐1 cells
Concentration: 0 μM; 0.1 μM; 1 μM; 10 μM; 50 μM; 100 μM
Incubation Time: 24 hours
Result: Induced autophagy in leukemia cells. 

体内研究
(In Vivo)

Pinosylvin (intravenous injection; 10 mg/kg) yields the plasma AUC, urine t , CL and Vd values of 5.23 ± 1.20 mgh mL-1, 13.13 ± 2.05 h, 1.84 ± 0.44 Lh-1kg-1 and 2.29 Lkg-1, respectively in male Sprague-Dawley rats, in a PK study[1].

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

分子量

212.24

Formula

C14H12O2

CAS 号

22139-77-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (471.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.7116 mL 23.5582 mL 47.1165 mL
5 mM 0.9423 mL 4.7116 mL 9.4233 mL
10 mM 0.4712 mL 2.3558 mL 4.7116 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 (protect from light)。-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 (11.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.78 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 (11.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.78 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 (11.78 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.78 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Lee SK, et al. Antibacterial and antifungal activity of pinosylvin, a constituent of pine.Fitoterapia. 2005 Mar;76(2):258-60.

    [2]. Roupe KA, et al. Pharmacokinetics of selected stilbenes: rhapontigenin, piceatannol and pinosylvin in rats.J Pharm Pharmacol. 2006 Nov;58(11):1443-50.

    [3]. Song J, et al. Pinosylvin enhances leukemia cell death via down-regulation of AMPKα expression. Phytother Res. 2018 Oct;32(10):2097-2104.

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Destruxin A

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。

Destruxin A 

Destruxin A(DA)是来源昆虫病原真菌 Metarhizium anisopliae 的环肽霉菌毒素,具有杀虫、抗病毒和抗增殖活性。

Destruxin A

Destruxin A Chemical Structure

CAS No. : 6686-70-0

规格 价格 是否有货
1 mg ¥8500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Destruxin A (DA) is a cyclo-peptidic mycotoxin from the entomopathogenic fungus Metarhizium anisopliae, with insecticidal, anti-viral and antiproliferative activities[1].

分子量

577.71

Formula

C29H47N5O7

CAS 号

6686-70-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Gong L, et al. Gene expression profile of Bombyx mori hemocyte under the stress of destruxin A. PLoS One. 2014 May 6;9(5):e96170.

    [2]. Pal S, et al. Fungal peptide Destruxin A plays a specific role in suppressing the innate immune response in Drosophila melanogaster. J Biol Chem. 2007 Mar 23;282(12):8969-77.

    [3]. Odier F, et al. In vitro effect of fungal cyclodepsipeptides on leukemic cells: study of destruxins A, B and E. Biol Cell. 1992;74(3):267-71.

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1,4-Naphthoquinone

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。

1,4-Naphthoquinone  纯度: 96.21%

1,4-Naphthoquinone 是抑制单胺氧化酶 MAO 和 DNA 拓扑异构酶活性的潜在药效基团,DNA 拓扑异构酶活性与抗肿瘤活性相关。

1,4-Naphthoquinone

1,4-Naphthoquinone Chemical Structure

CAS No. : 130-15-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥610 In-stock
100 mg ¥550 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

1,4-Naphthoquinone is a potential pharmacophore for inhibition of both MAO (monoamine oxidase) and DNA topoisomerase activities, this latter associated with antitumor activity[1].

分子量

158.16

Formula

C10H6O2

CAS 号

130-15-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (632.27 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 6.3227 mL 31.6136 mL 63.2271 mL
5 mM 1.2645 mL 6.3227 mL 12.6454 mL
10 mM 0.6323 mL 3.1614 mL 6.3227 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。-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 (15.81 mM); Clear solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (15.81 mM) 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 (15.81 mM); Clear solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (15.81 mM) 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
*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]. Coelho-Cerqueira E, et al. Beyond topoisomerase inhibition: antitumor 1,4-naphthoquinones as potential inhibitors of human monoamine oxidase. Chem Biol Drug Des. 2014 Apr;83(4):401-10.

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Zapnometinib(Synonyms: PD0184264; ATR-002)

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。

Zapnometinib (Synonyms: PD0184264; ATR-002) 纯度: 99.63%

Zapnometinib (PD0184264) 是 CI-1040 的活性代谢物,是一种 MEK 抑制剂,IC50 值为 5.7 nM。Zapnometinib 具有抗流感病毒的抗病毒活性和抗菌活性。

Zapnometinib(Synonyms: PD0184264;  ATR-002)

Zapnometinib Chemical Structure

CAS No. : 303175-44-2

规格 价格 是否有货 数量
5 mg ¥600 In-stock
10 mg ¥900 In-stock
25 mg ¥1100 In-stock
50 mg ¥2050 In-stock
100 mg ¥3950 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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  • Anti-Colorectal Cancer Compound Library

生物活性

Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities[1][2][3].

IC50 & Target[1]

MEK

5.7 nM (IC50)

体外研究
(In Vitro)

Zapnometinib (0.1 nM-1 μM) inhibits MEK, with IC50s of 30.96 nM, 357 nM, and 15 nM in cell free kinase assay, A549, MDCK cells and human PBMCs[1].
Zapnometinib (100 μM; 4 h) inhibits the Ionomycin (PMA/I)-induced phosphorylation of ERK1/2 in human PBMCs[1].
Zapnometinib (1-100 μM) reduces the viral titers of the IV H1N1pdm09, H3N2[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.

Western Blot Analysis[1]

Cell Line: human PBMCs
Concentration: 100 μM
Incubation Time: 4 h
Result: Inhibited the Ionomycin (PMA/I)-increased pERK1/2.

体内研究
(In Vivo)

Zapnometinib (8.4-75 mg/kg/day; three times a day p.o.) reduces the lung virus titers and enhances survival of mice after lethal H1N1pdm09 infection[1].
Zapnometinib (150 mg/kg) exhibits AUC values of 860.02 and 1953.68 μg•h/mL in mice by i.v. or oral route, respectively[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: Female C57BL/6 mice (8 weeks; 21-24 g) were infected with H1N1pdm09[1]
Dosage: 8.4, 25, 75 mg/kg/day (2.8, 8.4, 25 mg/kg)
Administration: P.o. three times a day
Result: Significantly reduced the virus titer at the dose of either 75 mg/kg/day or 25 mg/kg/day.

分子量

409.55

Formula

C13H7ClF2INO2

CAS 号

303175-44-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (152.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4417 mL 12.2085 mL 24.4170 mL
5 mM 0.4883 mL 2.4417 mL 4.8834 mL
10 mM 0.2442 mL 1.2209 mL 2.4417 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 (protect from light)。-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: ≥ 2.08 mg/mL (5.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.08 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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% corn oil

    Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.08 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 20.8 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]. Laure M, et, al. Antiviral efficacy against influenza virus and pharmacokinetic analysis of a novel MEK-inhibitor, ATR-002, in cell culture and in the mouse model. Antiviral Res. 2020 Jun;178:104806.

    [2]. Hamza H, et, al. Improved in vitro Efficacy of Baloxavir Marboxil Against Influenza A Virus Infection by Combination Treatment With the MEK Inhibitor ATR-002. Front Microbiol. 2021 Feb 12;12:611958.

    [3]. Bruchhagen C, et, al. Metabolic conversion of CI-1040 turns a cellular MEK-inhibitor into an antibacterial compound. Sci Rep. 2018 Jun 14;8(1):9114.

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Proglumide

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。

Proglumide  纯度: 99.40%

Proglumide 是一种非肽和口服活性胆囊收缩素 (CCK)-A/B 受体拮抗剂。Proglumide 选择性阻断 CCK 在中枢神经系统中的作用。Proglumide 具有抑制胃分泌和保护胃十二指肠粘膜的能力,还具有抗癫痫和抗氧化活性。

Proglumide

Proglumide Chemical Structure

CAS No. : 6620-60-6

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 ¥660 In-stock
50 mg ¥600 In-stock
100 mg ¥1100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities[1][2][3][4][5].

IC50 & Target

Cholecystokinin (CCK)-A/B receptors[1][2]

体外研究
(In Vitro)

In an in vitro study, Proglumide at concentrations between 0.3-10 mM inhibits CCK-stimulated amylase release dose-dependently, while Proglumide does not influence the basal amylase release at concentrations between 0-3 mM. Dose-response curves to CCK for amylase release shifted to the right with increase in Proglumide concentration. This inhibition by Proglumide is reversible. In addition, the effect of Proglumide is selective for CCK and its related peptide[2].
The incubation of HT29 cells with Proglumide significantly reduces the [3H]-thymidine incorporation to HT29 cells in a dose-dependent manner, with an IC50 of 6.5 mM. Proglumide reduces in a dose-dependent manner the percentage of necrosis with a parallel increase of apoptosis up to 70%[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.

体内研究
(In Vivo)

Proglumide (250-750 mg/kg; intraperitoneal injection; adult male Sprague Dawley rats) treatment is significantly effective in ameliorating the seizure activities, cognitive dysfunctions, and cerebral oxidative stress[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: Adult male Sprague Dawley rats (200-250 g; 2 months old) are induced status epilepticus (SE)[1]
Dosage: 250 mg/kg, 500 mg/kg, and 750 mg/kg
Administration: Intraperitoneal injection
Result: Dose-dependently and significantly increased the latencies to seizure and SE. Significantly and dose-dependently attenuated Li-PC (SE) induced increase in thiobarbituric acid (TBARS) and catalase (CAT), attenuated Li-Pc induced decrease in SOD, and attenuated depletion of GSH and glutathione-S transferase (GST) in the hippocampus and striatum.

Clinical Trial

分子量

334.41

Formula

C18H26N2O4

CAS 号

6620-60-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 65 mg/mL (194.37 mM)

* “≥” 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 2.9903 mL 14.9517 mL 29.9034 mL
5 mM 0.5981 mL 2.9903 mL 5.9807 mL
10 mM 0.2990 mL 1.4952 mL 2.9903 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。-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: ≥ 2.17 mg/mL (6.49 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (6.49 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 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: ≥ 2.17 mg/mL (6.49 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (6.49 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 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: ≥ 2.17 mg/mL (6.49 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (6.49 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 21.7 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]. Ahmad M, et al. The effects of quinacrine, proglumide, and pentoxifylline on seizure activity, cognitive deficit, and oxidative stress in rat lithium-pilocarpine model of status epilepticus. Oxid Med Cell Longev. 2014;2014:630509.

    [2]. Iwamoto Y, et al. In vitro and in vivo effect of proglumide on cholecystokinin-stimulated amylase release in mouse pancreatic acini. Gastroenterol Jpn. 1984 Feb;19(1):53-8.

    [3]. González-Puga C, et al. Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: synergism with pharmacological levels of melatonin. J Pineal Res. 2005 Oct;39(3):243-50.

    [4]. Bunney BS, et al. Further studies on the specificity of proglumide as a selective cholecystokinin antagonist in the central nervous system. Ann N Y Acad Sci. 1985;448:345-51.

    [5]. Tariq M, et al. Gastric and duodenal antiulcer and cytoprotective effects of proglumide in rats. J Pharmacol Exp Ther. 1987 May;241(2):602-7.

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Sesamol(Synonyms: 芝麻酚)

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。

Sesamol (Synonyms: 芝麻酚) 纯度: 99.93%

Sesamol 是芝麻油的主要成分,Sesamol 是一种自由基清除剂,在 DPPH 实验中,IC50 为 5.95±0.56 μg/mL。具有抗氧化活性。抗肿瘤活性。

Sesamol(Synonyms: 芝麻酚)

Sesamol Chemical Structure

CAS No. : 533-31-3

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 ¥550 In-stock
100 mg ¥500 In-stock
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生物活性

Sesamol is a constituent of sesame oil. Sesamol shows a free radical scavenging activity. Sesamol shows an IC50=5.95±0.56 μg/mL in the DPPH assay. Anti-oxidant activities[1]. Anticancer activities[2].

体外研究
(In Vitro)

Sesamol has also been shown to be a classical inhibitor of lipid peroxidation[1].
Sesamol (0-1 mM) efficiently induces the apoptosis of human liver hepatocellular carcinoma (HepG2) cells[2].
Sesamol suppresses cell proliferation and induces intrinsic and extrinsic apoptosis in HepG2 cells[2].
Sesamol treatment elicites mitochondrial dysfunction by inducing a loss of mitochondrial membrane potential. Sesamol inhibits mitophagy and autophagy through impeding the PI3K Class III/Belin-1 pathway. Sesamol decreases the expression of anti-apoptotic protein Bcl-2, but shows no effect on the expression of apoptotic signal Bax. Sesamol improves the protein expression of Fas/FasL, and activates tBid and caspase-8 which are all involved in the extrinsic apoptosis pathway[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)

Sesamol treatment for 35 days does not significantly impact body weight, although the tumor volume is dramatically inhibited (40.56% size inhibitory rate with Sesamol at 200 mg/kg compared to the control group). However, a lower dose (100 mg/kg Sesamol) only has significant anti-tumor growth effect up to 27 days after the first treatment[2].
The Bcl-2/Bax ratio in tumor tissues is also decreased. Moreover, in the Sesamol treatment group, levels of the cell proliferation marker Ki76 are down-regulated, and levels of the cell apoptosis marker cleaved-caspase 3 are increased when compared to control. The expression of LC3 protein is remarkably decreased by Sesamol in a dose-dependent manner[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

138.12

Formula

C7H6O3

CAS 号

533-31-3

中文名称

芝麻酚

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (724.01 mM)

Ethanol : ≥ 100 mg/mL (724.01 mM)

* “≥” 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 7.2401 mL 36.2004 mL 72.4008 mL
5 mM 1.4480 mL 7.2401 mL 14.4802 mL
10 mM 0.7240 mL 3.6200 mL 7.2401 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 (stored under nitrogen)。-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: ≥ 10 mg/mL (72.40 mM); Clear solution

    此方案可获得 ≥ 10 mg/mL (72.40 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 100.0 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: ≥ 10 mg/mL (72.40 mM); Clear solution

    此方案可获得 ≥ 10 mg/mL (72.40 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 100.0 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: ≥ 10 mg/mL (72.40 mM); Clear solution

    此方案可获得 ≥ 10 mg/mL (72.40 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 100.0 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: 10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (18.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (18.10 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 EtOH 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

  • 5.

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

    Solubility: ≥ 2.5 mg/mL (18.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (18.10 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 EtOH 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
  • 6.

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

    Solubility: ≥ 2.5 mg/mL (18.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (18.10 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 EtOH 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]. Kapadia GJ, et al. Chemopreventive effect of resveratrol, sesamol, sesame oil and sunflower oil in the Epstein-Barrvirus early antigen activation assay and the mouse skin two-stage carcinogenesis. Pharmacol Res. 2002 Jun;45(6):499-505.

    [2]. Liu Z, et al. Sesamol Induces Human Hepatocellular Carcinoma Cells Apoptosis by Impairing MitochondrialFunction and Suppressing Autophagy. Sci Rep. 2017 Apr 4;7:45728.

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4-Hydroxylonchocarpin

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。

4-Hydroxylonchocarpin  纯度: ≥96.0%

4-Hydroxylonchocarpin 是一种查尔酮化合物,来自补骨脂 (Psoralea corylifolia) 提取物。4-Hydroxylonchocarpin 增强 p38 MAPK,JNK 和 ERK 的磷酸化。4-Hydroxylonchocarpin 具有多种药理活性,包括抗菌,抗癌,抗逆转录酶,抗结核,抗疟,抗炎和抗氧化活性。

4-Hydroxylonchocarpin

4-Hydroxylonchocarpin Chemical Structure

CAS No. : 56083-03-5

规格 价格 是否有货 数量
5 mg ¥3030 In-stock
10 mg ¥5140 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

4-Hydroxylonchocarpin is a chalcone compound from an extract of Psoralea corylifolia. 4-Hydroxylonchocarpin increases phosphorylation of p38 MAPK, JNK and ERK. 4-Hydroxylonchocarpin has diverse pharmacological activities, including antibacterial, antifungal, anticancer, antireverse transcriptase, antitubercular, antimalarial, anti-inflammatory and antioxidant activities[1].

分子量

322.35

Formula

C20H18O4

CAS 号

56083-03-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (155.11 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1022 mL 15.5111 mL 31.0222 mL
5 mM 0.6204 mL 3.1022 mL 6.2044 mL
10 mM 0.3102 mL 1.5511 mL 3.1022 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 (protect from light)。-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 (7.76 mM); Clear solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.76 mM) 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 (7.76 mM); Clear solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.76 mM) 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
*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]. Lim J, et al. Antimelanogenic effect of 4-hydroxylonchocarpin through the inhibition of tyrosinase-related proteins and MAPK phosphatase. Exp Dermatol. 2016 Jul;25(7):574-6.

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Hypocrellin B

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。

Hypocrellin B  纯度: 98.12%

Hypocrellin B 是从真菌Hypocrella bambusaeShiraia bambusicola 中分离得到的一种色素,是一个凋亡诱导剂。Hypocrellin B 是一种光敏剂,可用于癌症光动力研究。Hypocrellin B 还拥有抗菌和抗利什曼活性。

Hypocrellin B

Hypocrellin B Chemical Structure

CAS No. : 123940-54-5

规格 价格 是否有货 数量
5 mg ¥2520 In-stock
10 mg ¥4290 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

Hypocrellin B, a pigment isolated from the fungi Hypocrella bambusae and Shiraia bambusicola, is an apoptosis inducer. Hypocrellin B can be used as a photosensitizer for photodynamic therapy of cancer. Hypocrellin B also has antimicrobial and antileishmanial activities[1][2][3].

分子量

528.51

Formula

C30H24O9

CAS 号

123940-54-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 2 mg/mL (3.78 mM; Need ultrasonic)

*Hypocrellin B is usually formulated as a suspension.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8921 mL 9.4606 mL 18.9211 mL
5 mM
10 mM

*

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 (protect from light)。-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]. Miller GG, et al. Preclinical assessment of hypocrellin B and hypocrellin B derivatives as sensitizers for photodynamic therapy of cancer: progress update. Photochem Photobiol. 1997 Apr;65(4):714-22.

    [2]. Wang X, et al. Hypocrellin B-mediated sonodynamic action induces apoptosis of hepatocellular carcinoma cells. Ultrasonics. 2012 Apr;52(4):543-6.

    [3]. Ma G, et al. Antimicrobial and antileishmanial activities of hypocrellins A and B. Antimicrob Agents Chemother. 2004 Nov;48(11):4450-2.

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Trifolirhizin(Synonyms: 三叶豆紫檀苷)

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。

Trifolirhizin (Synonyms: 三叶豆紫檀苷) 纯度: 99.91%

Trifolirhizin 是从苦参根中分离出的一种 pterocarpan 黄酮类化合物。Trifolirhizin 具有高效的 tyrosinase 抑制活性,IC50 为 506 μM。Trifolirhizin 具有潜在的抗炎和抗癌活性。

Trifolirhizin(Synonyms: 三叶豆紫檀苷)

Trifolirhizin Chemical Structure

CAS No. : 6807-83-6

规格 价格 是否有货 数量
5 mg ¥990 In-stock
10 mg ¥1680 In-stock
20 mg ¥2860 In-stock
50 mg   询价  
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生物活性

Trifolirhizin is a pterocarpan flavonoid isolated from the roots of Sophora flavescens. Trifolirhizin possesses potent tyrosinase inhibitory activity with an IC50 of 506 μM[1]. Trifolirhizin exhibits potential anti-inflammatory and anticancer activities[2].

IC50 & Target

IC50: 506 μM (tyrosinase)[1]

分子量

446.40

Formula

C22H22O10

CAS 号

6807-83-6

中文名称

三叶豆紫檀苷

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献
  • [1]. Hyun SK, et al. Inhibitory effects of kurarinol, kuraridinol, and trifolirhizin from Sophora flavescens on tyrosinase and melanin synthesis. Biol Pharm Bull. 2008 Jan;31(1):154-8.

    [2]. Zhou H, et al. Anti-Inflammatory and antiproliferative activities of trifolirhizin, a flavonoid from Sophora flavescens roots. J Agric Food Chem. 2009 Jun 10;57(11):4580-5.

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Cyclapolin 9

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。

Cyclapolin 9  纯度: 96.13%

Cyclapolin 9 是一种有效的,选择性的和 ATP 竞争性 polo-like kinase 1 (PLK1) 抑制剂,IC50 为 500 nM,对其他激酶没有活性。

Cyclapolin 9

Cyclapolin 9 Chemical Structure

CAS No. : 40533-25-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3850 In-stock
5 mg ¥3500 In-stock
10 mg   询价  
50 mg   询价  

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生物活性

Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1 (PLK1) inhibitor with an IC50 of 500 nM. Cyclapolin 9 is inactive against other kinases[1][2].

IC50 & Target[2]

PLK1

500 nM (IC50)

体外研究
(In Vitro)

Cyclapolin 9 (3 μM) reduces electric field stimulation (EFS)-induced contractions of prostate strips. The α1-adrenergic smooth muscle contraction in the human prostate can be inhibited by Cyclapolin 9[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.

分子量

307.21

Formula

C9H4F3N3O4S

CAS 号

40533-25-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (16.28 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2551 mL 16.2755 mL 32.5510 mL
5 mM 0.6510 mL 3.2551 mL 6.5102 mL
10 mM 0.3255 mL 1.6276 mL 3.2551 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。-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]. Martin Hennenberg, et al. Inhibition of Prostate Smooth Muscle Contraction by Inhibitors of Polo-Like Kinases. Front Physiol. 2018 Jun 15;9:734.

    [2]. Campbell McInnes, et al. Inhibitors of Polo-like kinase reveal roles in spindle-pole maintenance. Nat Chem Biol. 2006 Nov;2(11):608-17.

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N-Desmethyl-Apalutamide

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。

N-Desmethyl-Apalutamide  纯度: 97.24%

N-Desmethyl Apalutamide 是 Apalutamide 的活性代谢产物,是一种低活性的雄激素受体拮抗剂,其作用力是 Apalutamide 活性的三分之一。N-Desmethyl Apalutamide 的形成主要由 CYP2C8 和 CYP3A4 介导。N-Desmethyl Apalutamide 是中等至强的 CYP3A4CYP2B6 诱导剂,并具有优异的血浆蛋白结合浓度。

N-Desmethyl-Apalutamide

N-Desmethyl-Apalutamide Chemical Structure

CAS No. : 1332391-11-3

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  • Bioactive Compound Library Plus

生物活性

N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration[1][2][3].

IC50 & Target

CYP3A4 and CYP2B6[1]; Androgen receptor[2]

分子量

463.41

Formula

C20H13F4N5O2S

CAS 号

1332391-11-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Pérez-Ruixo C, et al. Population Pharmacokinetics of Apalutamide and its Active Metabolite N-Desmethyl-Apalutamide in Healthy and Castration-Resistant Prostate Cancer Subjects. Clin Pharmacokinet. 2019 Aug 20.

    [2]. Smith MR, et al. Phase 2 Study of the Safety and Antitumor Activity of Apalutamide (ARN-509), a Potent Androgen Receptor Antagonist, in the High-risk Nonmetastatic Castration-resistant Prostate Cancer Cohort. Eur Urol. 2016 May 6. pii: S0302-2838(16)30133

    [3]. May MB, et al. Apalutamide: A new agent in the management of prostate cancer. J Oncol Pharm Pract. 2019 Dec;25(8):1968-1978.

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LY2334737

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。

LY2334737  纯度: 99.02%

LY2334737 是一种核苷类似物,也是一种具有口服活性的 Gemcitabine 的前药。LY2334737 对肠道病毒 A71 (EV-A71) 感染具有抑制活性。LY2334737 具有抗病毒和抗癌作用。

LY2334737

LY2334737 Chemical Structure

CAS No. : 892128-60-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1880 In-stock
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5 mg ¥2195 In-stock
10 mg ¥3348 In-stock
50 mg ¥7952 In-stock
100 mg ¥12369 In-stock
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LY2334737 相关产品

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  • Anti-Cancer Metabolism Compound Library

生物活性

LY2334737 is an nucleoside analog and is an orally active prodrug of Gemcitabine. LY2334737 exhibits inhibitory activity against enterovirus A71 (EV-A71) infection. LY2334737 has antiviral and anticancer effects[1][2].

IC50 & Target

Enterovirus A71 (EV-A71)[2]

体外研究
(In Vitro)

Five cell lines that express CES2 responded to LY2334737 treatment. LY2334737 is less cytotoxic to a SK-OV-3 CES2 knockdown than parental cells. The drug response of CES2-transfected HCT-116 cells correlated with CES2 expression level. Bystander studies show statistically greater PC-3-GFP growth inhibition by LY2334737 when cells are cocultured with CES2 and not mock transfectants[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)

Oral treatment of xenograft models with 3.2 mg/kg LY2334737 once a day for 21 days shows greater tumor growth inhibition of CES2 transfectant than the mock transfectant[1].
Metronomic LY2334737 administration causes increased blood flow in luciferase-tagged LM2-4 tumor xenografts, and this effect, readily measured using contrast micro-ultrasound, coincided with a relative increase in tumor bioluminescence[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

389.39

Formula

C17H25F2N3O5

CAS 号

892128-60-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (256.81 mM)

* “≥” 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 2.5681 mL 12.8406 mL 25.6812 mL
5 mM 0.5136 mL 2.5681 mL 5.1362 mL
10 mM 0.2568 mL 1.2841 mL 2.5681 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。-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 (6.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.42 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 (6.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.42 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 (6.42 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.42 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]. Pratt SE, et al. Human carboxylesterase-2 hydrolyzes the prodrug of gemcitabine (LY2334737) and confers prodrug sensitivity to cancer cells. Clin Cancer Res. 2013 Mar 1;19(5):1159-68.

    [2]. Jialei Sun, et al. Drug Repurposing of Pyrimidine Analogs as Potent Antiviral Compounds Against Human Enterovirus A71 Infection With Potential Clinical Applications. Sci Rep. 2020 May 18;10(1):8159.

    [3]. Francia G, et al. Low-dose metronomic oral dosing of a prodrug of gemcitabine (LY2334737) causes antitumor effects in the absence of inhibition of systemic vasculogenesis. Mol Cancer Ther. 2012 Mar;11(3):680-9.

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Abacavir monosulfate(Synonyms: 阿巴卡韦单硫酸盐)

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。

Abacavir monosulfate (Synonyms: 阿巴卡韦单硫酸盐)

Abacavir monosulfate 是一种竞争性的口服活性核苷逆转录酶(nucleoside reverse transcriptase)抑制剂。 Abacavir monosulfate 可抑制 HIV 的复制。Abacavir monosulfate 在前列腺癌细胞系中显示出抗癌活性。Abacavir monosulfate 可突破血脑屏障,抑制端粒酶(telomerase)活性。

Abacavir monosulfate(Synonyms: 阿巴卡韦单硫酸盐)

Abacavir monosulfate Chemical Structure

CAS No. : 216699-07-9

规格 是否有货
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Abacavir monosulfate 的其他形式现货产品:

Abacavir Abacavir sulfate

生物活性

Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity[1][2][3].

体外研究
(In Vitro)

Abacavir (15 and 150 μM, 0-120 h) monosulfate inhibits cell growth, affects cell cycle progression, induces senescence and modulates LINE-1 mRNA expression in prostate cancer cell lines[1].
Abacavir (15 and 150 μM, 18 h) monosulfate significantly reduces cell migration and inhibits cell invasion[1].
Abacavir monsulfate induces fat apoptosis[4].

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

Cell Proliferation Assay[1]

Cell Line: PC3, LNCaP and WI-38
Concentration: 15 and 150 μM
Incubation Time: 0, 24, 48, 72 and 96 h
Result: Showed a dose-dependent growth inhibition on PC3 and LNCaP.

Cell Cycle Analysis[1]

Cell Line: PC3 and LNCaP
Concentration: 150 μM
Incubation Time: 0, 18, 24, 48, 72, 96 and 120 h
Result: Caused a very high accumulation of cells in S phase in PC3 and LNCaP cells, and G2/M phase increment was observed in PC3 cells.

Cell Migration Assay [1]

Cell Line: PC3 and LNCaP
Concentration: 15 and 150 μM
Incubation Time: 18 h
Result: Significantly reduced cell migration.

Cell Invasion Assay[1]

Cell Line: PC3 and LNCaP
Concentration: 15 and 150 μM
Incubation Time: 18 h
Result: Significantly inhibited cell invision.

体内研究
(In Vivo)

Abacavir (0-7.5 μg/mL, 100 μL, intrascrotal administration; 100 and 200 mg/kg, p.o.; 4 h) monosulfate dose-dependently promoted thrombus formation[2].
Abacavir (50 mg/kg/d; i.p.; 14 days) monosulfate with 0.1 mg/kg/d Decitabine (HY-A0004) enhances survival of high-risk medulloblastoma-bearing mice[3].

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

Animal Model: Male mice (9-weeks old, 22-30 g) – wild-type (WT) C57BL/6 or homozygous knockout (P2rx7 KO, B6.129P2-P2rx7tm1Gab/J)[2]
Dosage: 2.5, 5 and 7.5 μg/mL, 100 μL or 100 and 200 mg/kg
Administration: Intrascrotal or oral administration for 4 h
Result: Dose-dependently promoted thrombus formation.
Animal Model: NSGTM mice, patient-derived xenograft (PDX) cells of non-WNT/non-SHH, Group 3 and of SHH/ TP53-mutated medulloblastoma[3]
Dosage: 50 mg/kg/d with 0.1 mg/kg/d Decitabine
Administration: Intraperitoneal injection, daily for 14 days
Result: Inhibited tumor growth and enhanced mouse survival.

分子量

384.41

Formula

C14H20N6O5S

CAS 号

216699-07-9

中文名称

阿巴卡韦单硫酸盐

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]. Carlini F, et al. The reverse transcription inhibitor abacavir shows anticancer activity in prostate cancer cell lines. PLoS One. 2010 Dec 3;5(12):e14221.

    [2]. Collado-Diaz V, et al. Abacavir Induces Arterial Thrombosis in a Murine Model. J Infect Dis. 2018 Jun 20;218(2):228-233.

    [3]. Gringmuth M, et al. Enhanced Survival of High-Risk Medulloblastoma-Bearing Mice after Multimodal Treatment with Radiotherapy, Decitabine, and Abacavir. Int J Mol Sci. 2022 Mar 30;23(7):3815.

    [4]. McComsey GA, et al. Improvements in lipoatrophy, mitochondrial DNA levels and fat apoptosis after replacing stavudine with abacavir or zidovudine. AIDS. 2005 Jan 3;19(1):15-23.

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PD-1/PD-L1-IN-9

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。

PD-1/PD-L1-IN-9  纯度: 98.01%

PD-1/PD-L1-IN-9 是一种有效和具有口服活性的 PD-1/PD-L1 相互作用抑制剂,IC50 值为 3.8 nM。PD-1/PD-L1-IN-9 可以增强免疫细胞对肿瘤细胞的杀伤活性。PD-1/PD-L1-IN-9 在 CT26 小鼠模型中表现出显着的体内抗肿瘤活性。

PD-1/PD-L1-IN-9

PD-1/PD-L1-IN-9 Chemical Structure

CAS No. : 2628506-54-5

规格 价格 是否有货 数量
5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
25 mg ¥11000 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model[1].

IC50 & Target

IC50: 3.8 nM (PD-1/PD-L1)[1]

体外研究
(In Vitro)

PD-1/PD-L1-IN-9 (compound 24) (46.9-1500 nM; pretreated for 2 h) dose-dependently significantly activates the antitumor immunity of PBMCs to MDB-MB 231 cells, with an EC50 of ∼100 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)

PD-1/PD-L1-IN-9 (compound 24) (40-80 mg/kg; p.o. once a day for 2 weeks) inhibits tumor growth in a dose-dependent manner and does not cause any body weight loss or mortality of mice[1].
PD-1/PD-L1-IN-9 (3 mg/kg; a single i.v.) exhibits half-life (t1/2=4.2 h), plasma clearance (Cl=11.5 L/h/kg) and Cmax (1233 ng/mL) in rats[1].
PD-1/PD-L1-IN-9 (25 mg/kg; a single p.o.) exhibits moderate oral bioavailability (F=22 %), half-life (t1/2=6.4 h) and Cmax (192 ng/mL) in rats[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: Male BALB/c mice (5-6 weeks) were inoculated CT26 cells[1]
Dosage: 40, 80 mg/kg
Administration: P.o. once a day for 2 weeks
Result: Significantly decreased the final tumor weight, with TGI values of 60 and 67% at the dose of 40 and 80 mg/kg, respectively.
Animal Model: Sprague-Dawley (SD) rats[1]
Dosage: 3 mg/kg for i.v. and 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: A single i.v. or p.o.
Result: I.v.: t1/2=4.2 h; Cl=11.5 L/h/kg; Cmax=1233 ng/mL.
P.o.: F=22 %; t1/2=6.4 h; Cmax=192 ng/mL.

分子量

348.44

Formula

C22H24N2O2

CAS 号

2628506-54-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (286.99 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8699 mL 14.3497 mL 28.6993 mL
5 mM 0.5740 mL 2.8699 mL 5.7399 mL
10 mM 0.2870 mL 1.4350 mL 2.8699 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。-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 (7.17 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.17 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 (7.17 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.17 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 (7.17 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.17 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]. Wang T, et, al. Novel Biphenyl Pyridines as Potent Small-Molecule Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction. J Med Chem. 2021 May 30.

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JMJD7-IN-1

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。

JMJD7-IN-1  纯度: 98.07%

JMJD7-IN-1 是一种有效的 JMJD7 抑制剂,IC50 值为 6.62 μM。JMJD7-IN-1 对表达高水平 JMJD7 的细胞显示出良好的抑制活性。

JMJD7-IN-1

JMJD7-IN-1 Chemical Structure

CAS No. : 311316-96-8

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 ¥1100 In-stock
5 mg ¥1000 In-stock
10 mg ¥1700 In-stock
25 mg ¥3500 In-stock
50 mg ¥5500 In-stock
100 mg ¥9500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

JMJD7-IN-1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library

生物活性

JMJD7-IN-1 is a potent JMJD7 inhibitor, with an IC50 of 6.62 μM. JMJD7-IN-1 shows good inhibitory activity against cells expressing a high level of JMJD7[1].

IC50 & Target

IC50: 6.62 μM (JMJD7)[1]

体外研究
(In Vitro)

JMJD7-IN-1 (0.1-1000 μM) dose-dependently inhibits the activity of JMJD7, with an IC50 of 6.62 μM[1].
JMJD7-IN-1 efficiently binds to JMJD7, with an IC50 of 3.80 μM[1].
JMJD7-IN-1 (72 h) inhibits the growth of T-47d, SK-BR-3, Jurkat and Hela cells, with IC50s of 9.40 μM, 13.26 μM, 15.03 μM and 16.14 μM, respectively[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.

分子量

363.15

Formula

C16H8Cl2N2O4

CAS 号

311316-96-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 8.33 mg/mL (22.94 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7537 mL 13.7684 mL 27.5368 mL
5 mM 0.5507 mL 2.7537 mL 5.5074 mL
10 mM 0.2754 mL 1.3768 mL 2.7537 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 (protect from light)。-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]. Zhang W, et, al. Discovery of JMJD7 inhibitors with the aid of virtual screening and bioactivity evaluation. Bioorg Med Chem Lett. 2021 May 25;45:128139.

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4(3H)-Quinazolinone

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。

4(3H)-Quinazolinone  纯度: 99.91%

4(3H)-Quinazolinone是化学合成中的砌块。 生物活性氮杂环化合物。 具有广谱的生物学特性,如抗菌,抗真菌,抗惊厥,抗炎,抗HIV,抗癌和缓解疼痛活性。

4(3H)-Quinazolinone

4(3H)-Quinazolinone Chemical Structure

CAS No. : 491-36-1

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

* Please select Quantity before adding items.

4(3H)-Quinazolinone 相关产品

相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Immunology/Inflammation Compound Library
  • Natural Product Library
  • Anti-Cancer Compound Library
  • Fragment Library
  • Endocrinology Compound Library
  • Antibacterial Compound Library
  • Traditional Chinese Medicine Monomer Library
  • Alkaloids Library

生物活性

4(3H)-Quinazolinone is a building block in chemical synthesis. Biologically active nitrogen heterocyclic compounds. Possesses a wide spectrum of biological properties like antibacterial, antifungal, anticonvulsant, anti-inflammatory, anti-HIV, anticancerous and analgesic activities[1][2].

分子量

146.15

Formula

C8H6N2O

CAS 号

491-36-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 110 mg/mL (752.65 mM; Need ultrasonic)

H2O : 1.2 mg/mL (8.21 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 6.8423 mL 34.2114 mL 68.4229 mL
5 mM 1.3685 mL 6.8423 mL 13.6846 mL
10 mM 0.6842 mL 3.4211 mL 6.8423 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。-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: ≥ 2.75 mg/mL (18.82 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (18.82 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 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: ≥ 2.75 mg/mL (18.82 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (18.82 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 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: ≥ 2.75 mg/mL (18.82 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (18.82 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 27.5 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]. Jafari E, et al. Quinazolinone and quinazoline derivatives: recent structures with potent antimicrobial and cytotoxic activities. Res Pharm Sci. 2016 Jan-Feb;11(1):1-14.

    [2]. Hameed A, et al. Quinazoline and quinazolinone as important medicinal scaffolds: a comparative patent review (2011-2016). Expert Opin Ther Pat. 2018 Apr;28(4):281-297.

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