标签归档：nk

Pitavastatin D4(Synonyms: NK-104 D4)

发表于由

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。

Pitavastatin D4 (Synonyms: NK-104 D4)

Pitavastatin D4 (NK-104 D4) 是 Pitavastatin 的氘代物。Pitavastatin 是一种有效的 HMG-CoA 还原酶抑制剂。

Pitavastatin D4(Synonyms: NK-104 D4)

Pitavastatin D4 Chemical Structure

CAS No. : 2070009-71-9

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生物活性

Pitavastatin D4 (NK-104 D4) is deuterium labeled Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.

分子量

425.49

Formula

C25H20D4FNO4
CAS 号

2070009-71-9
中文名称

匹伐他汀 D4
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.

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

Pitavastatin D4(Synonyms: NK-104 D4)

发表于由

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。

Pitavastatin D4 (Synonyms: NK-104 D4)

Pitavastatin D4 (NK-104 D4) 是 Pitavastatin 的氘代物。Pitavastatin 是一种有效的 HMG-CoA 还原酶抑制剂。

Pitavastatin D4(Synonyms: NK-104 D4)

Pitavastatin D4 Chemical Structure

CAS No. : 2070009-71-9

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

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生物活性

Pitavastatin D4 (NK-104 D4) is deuterium labeled Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.

分子量

425.49

Formula

C25H20D4FNO4
CAS 号

2070009-71-9
中文名称

匹伐他汀 D4
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.

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

SN-38(Synonyms: NK012)

发表于由

SN-38 (Synonyms: NK012) 纯度: 99.80%

SN-38 (NK012) 是拓扑异构酶 I (Topoisomerase I) 抑制剂伊立替康的活性代谢产物。SN-38 (NK012) 抑制 DNA 合成和 RNA 合成的 IC50 分别为 0.077 和 1.3 μM。

SN-38(Synonyms: NK012)

SN-38 Chemical Structure

CAS No. : 86639-52-3

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 ￥825 In-stock
50 mg ￥750 In-stock
100 mg ￥990 In-stock
500 mg ￥1480 In-stock
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5 g   询价  

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生物活性

SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively[1][2][3][4].

IC50 & Target[1]

Topoisomerase I

 

Camptothecins

 

体外研究
(In Vitro)

The IC50 values for LoVo, HCT116, and HT29 cell lines is 20 nM, 50 nM, 130 nM, respectively. In all three SN-38 (NK012) resistant cell lines Top1 activity is maintained in the presence of high concentrations of SN-38[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

SN-38 (NK012), the active and toxic metabolite of the anticancer prodrug Irinotecan. At 30 minutes after administration, Irinotecan plasma concentrations in Slco1a/1b(−/−) mice are 1.9-fold higher than in the wild-type mice (1.89 vs. 1.01 μM, respectively), whereas SN-38 (NK012) plasma concentrations of Slco1a/1b(−/−) mice are 8-fold higher compare with wild-type mice (0.4 μg/mL vs. 0.05 μg/mL, respectively). Overall plasma exposure [AUC(5-240)] of Irinotecan is 1.7-fold higher in Oatp1a/1b knockout mice versus wild-type mice (209.8±6.7 vs. 120.9±4.4 μM/min; P<0.01), and 2.9-fold higher for SN-38 (50±2.9 vs. 12±2 μM/min; P<0.001)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

392.40

Formula

C22H20N2O5
CAS 号

86639-52-3
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 : 50 mg/mL (127.42 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 2.5484 mL 12.7421 mL 25.4842 mL
5 mM 0.5097 mL 2.5484 mL 5.0968 mL
10 mM 0.2548 mL 1.2742 mL 2.5484 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% corn oil

    Solubility: 2.5 mg/mL (6.37 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.37 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玉米油中，混合均匀。

  • 2.

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

    Solubility: 2.08 mg/mL (5.30 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.30 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 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

  • 3.

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

    Solubility: 2.08 mg/mL (5.30 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.30 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 20.8 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 MCE 网站选购。
参考文献

  • [1]. Wallin A, et al. Anticancer effect of SN-38 on colon cancer cell lines with different metastatic potential. Oncol Rep. 2008 Jun;19(6):1493-8.

    [2]. Jensen NF, et al. Characterization of DNA topoisomerase I in three SN-38 resistant human colon cancer cell lines reveals a newpair of resistance-associated mutations. J Exp Clin Cancer Res. 2016 Mar 31;35:56.

    [3]. Kawato Y, et al. Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11. Cancer Res. 1991;51(16):4187-4191.
Cell Assay
[2]

In vitro SN-38 (NK012) sensitivity is determined using the MTT assay. Cells are seeded in 96-well plates, and a range of SN-38 (NK012) concentrations is added the following day. Following 48 h of drug exposure, the medium is discarded and the plates are incubated with medium containing MTT (0.5 mg/mL) for 3 h. Acidified (0.02 M HCl) sodium dodecyl sulphate (20 %) is added to dissolve the formed formazan. Optical density at 570 nm (and 670 nm for background) is measured, and the cell viability is calculated in percent compared to untreated cells. Experiments are repeated three times and the mean IC50 value ± standard deviation is determined. Relative resistance for each resistant cell line is calculated by dividing the mean IC50 value of the resistant cell line by the mean IC50 value of the corresponding parental cell line[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
Female wild-type, Slco1a/1b(−/−)(Oatp1a/1b knockout), Slco1a/1b(−/−);1B1(tg), and Slco1a/1b(−/−);1B3(tg) (liver-specific OATP1B1 and OATP1B3 humanized transgenic) mice of comparable genetic background (>99% FVB) between 8 and 14 weeks of age are used. Irinotecan (20 mg/mL in water-based solution containing NaOH, lactic acid, and sorbitol) is diluted with saline (to 2 mg/mL) for administration of 10 mg/kg; 5 μL/g bodyweight are administered intravenously to mice. SN-38 (NK012) is dissolved in DMSO (1 mg/mL) and 1 μL/g body weight is administered intravenously to mice to achieve a dosage of 1 mg/kg. The experiments are terminated by isoflurane anaesthesia, heparin-blood sampling by cardiac puncture followed by cervical dislocation and tissue collection. Blood samples are centrifuged at 5,200 × g for 5 minutes at 4°C and plasma is collected and stored at −30°C until analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Wallin A, et al. Anticancer effect of SN-38 on colon cancer cell lines with different metastatic potential. Oncol Rep. 2008 Jun;19(6):1493-8.

    [2]. Jensen NF, et al. Characterization of DNA topoisomerase I in three SN-38 resistant human colon cancer cell lines reveals a newpair of resistance-associated mutations. J Exp Clin Cancer Res. 2016 Mar 31;35:56.

    [3]. Kawato Y, et al. Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11. Cancer Res. 1991;51(16):4187-4191.

GR 159897

发表于由

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。

GR 159897 

GR 159897 是一种高效，选择性，竞争性，可通过血脑屏障的非肽神经激肽 2 (NK2) 受体拮抗剂。GR 159897 对 NK1 和 NK3 受体几乎没有亲和力。GR 159897 抑制 [3H]GR100679 与人 NK2-CHO 细胞和大鼠结肠膜的结合，pKi 值分别为 9.51 和 10。拮抗支气管收缩。抗焦虑和抗肿瘤作用。

GR 159897

GR 159897 Chemical Structure

CAS No. : 158848-32-9

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生物活性

GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects[1][2].

IC50 & Target[1]

NK2

10 (pKi, Rat colon membrane)

hNK2

9.51 (pKi, CHO cell)

体外研究
(In Vitro)

GR 159897 (10-30 μM; 72 hours; 4T1, 4THM, 4TLM and 67NR cells) treatment inhibits proliferation of cells in all cell lines dose- dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells[2].
GR 159897 (10-30 μM; 72 hours; 4TBM, 4TLM, 4THM and 4T1 cells) treatment increases phosphorylation of P38, while inhibiting AKT activation in all metastatic cell lines whereas phosphorylation of ERK decreased in 4TBM, 4TLM and 4THM but not in 4T1 cells[2].

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

Cell Proliferation Assay[2]

Cell Line: 4T1, 4THM, 4TLM and 67NR cells
Concentration: 10 μM, 30 μM
Incubation Time: 72 hours
Result: Inhibited proliferation of cells in all cell lines dose- dependently, a response more pronounced in 4T1, 4THM and 4TLM cells compared to 67NR cells.

Western Blot Analysis[2]

Cell Line: 4TBM, 4TLM, 4THM and 4T1 cells
Concentration: 10 μM, 30 μM
Incubation Time: 40 hours
Result: Increased phosphorylation of P38.

体内研究
(In Vivo)

GR 159897 (0.12 mg/kg; intravenous injection; guinea-pigs) treatment potently antagonizes bronchoconstriction induced by GR64349, with a long duration of action (3 h)[1].

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

Animal Model: Guinea-pigs[1]
Dosage: 0.12 mg/kg
Administration: Intravenous injection
Result: Potently antagonised bronchoconstriction induced by GR64349, with a long duration of action (3 h).

分子量

414.54

Formula

C23H27FN2O2S
CAS 号

158848-32-9
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]. Beresford IJ, et al. GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur J Pharmacol. 1995 Jan 16;272(2-3):241-8.

    [2]. Nizam E, et al. Differential consequences of neurokinin receptor 1 and 2 antagonists in metastatic breast carcinoma cells; Effects independent of Substance P. Biomed Pharmacother. 2018 Dec;108:263-270.

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Pitavastatin(Synonyms: 匹伐他汀; NK-104)

发表于由

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。

Pitavastatin (Synonyms: 匹伐他汀; NK-104)

Pitavastatin (NK-104) 是有效的羟甲基戊二酰-CoA (HMG-CoA) 还原酶抑制剂。Pitavastatin 在 HepG2 细胞中抑制乙酸合成胆固醇的 IC50 为 5.8 nM。Pitavastatin 是一种高效的肝细胞低密度脂蛋白胆固醇 (LDL-C) 受体诱导剂。具有抗癌活性。

Pitavastatin(Synonyms: 匹伐他汀; NK-104)

Pitavastatin Chemical Structure

CAS No. : 147511-69-1

规格 是否有货
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250 mg   询价  
500 mg   询价  

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Pitavastatin 的其他形式现货产品:

Pitavastatin Calcium

生物活性

Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.

体外研究
(In Vitro)

Pitavastatin inhibits the growth of a panel of ovarian cancer cells, including those considered most likely to represent HGSOC, grown as a monolayers (IC50=0.4-5 μM) or as spheroids (IC50 = 0.6-4 μM)[4]. 
Pitavastatin (1 μM; 48 hours ) induces apoptosis, evidenced by the increased activity of executioner caspases-3,7 as well as caspase-8 and caspase-9 in Ovcar-8 cells and Ovcar-3 cells[4].
Pitavastatin (1 μM, 48 hours) caused PARP cleavage in Ovcar-8 cells[4].

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

Western Blot Analysis[1]

Cell Line: Ovcar-8 cells
Concentration: 1 μM
Incubation Time: 48 hours
Result: Induced PARP cleavage.

体内研究
(In Vivo)

Pitavastatin (59 mg/kg; p.o.; twice daily for 28 days) caused significant tumour regression[4].

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

Animal Model: 4 week old female NCR Nu/Nu female mice (bearing Ovcar-4 tumours)[4]
Dosage: 59 mg/kg
Administration: p.o.; twice daily for 28 days
Result: Caused significant tumour regression.

Clinical Trial

分子量

421.46

Formula

C25H24FNO4
CAS 号

147511-69-1
中文名称

匹伐他汀
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]. Morikawa S, et al. Relative induction of mRNA for HMG CoA reductase and LDL receptor by five different HMG-CoA reductase inhibitors in cultured human cells. J Atheroscler Thromb. 2000;7(3):138-44.

    [2]. Katsuki S, et al. Nanoparticle-mediated delivery of pitavastatin inhibits atherosclerotic plaque destabilization/rupture in mice by regulating the recruitment of inflammatory monocytes. Circulation. 2014 Feb 25;129(8):896-906.

    [3]. Tajiri K, et al. Pitavastatin regulates helper T-cell differentiation and ameliorates autoimmune myocarditis in mice. Cardiovasc Drugs Ther. 2013 Oct;27(5):413-24.

    [4]. Hamano T, et al. Pitavastatin decreases tau levels via the inactivation of Rho/ROCK. Neurobiol Aging. 2012 Oct;33(10):2306-20.

    [5]. de Wolf E, et al.Dietary geranylgeraniol can limit the activity of pitavastatin as a potential treatment for drug-resistant ovarian cancer.Sci Rep. 2017 Jul 14;7(1):5410.

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

L-732138

发表于由

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-732138  纯度: 99.43%

L-732138 是一种选择性，有效和竞争性神经激肽-1 (NK-1) 受体拮抗剂，IC50 为 2.3 nM。L-732138 在克隆的人 NK-1 受体中的效力比在克隆大鼠 NK-1 受体中高 200 倍，比人类 NK-2 和 NK-3 受体高 1000 倍以上。L-732138 可减轻痛觉过敏并具有抗肿瘤作用。

L-732138

L-732138 Chemical Structure

CAS No. : 148451-96-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2962 In-stock
1 mg ￥850 In-stock
5 mg ￥2850 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

L-732138 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Neuronal Signaling Compound Library
  • Anti-Cancer Compound Library
  • Neurotransmitter Receptor Compound Library
  • Targeted Diversity Library

生物活性

L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action[1][2].

IC50 & Target[1][2]

NK1

2.3 nM (IC50)

体外研究
(In Vitro)

L-732138 (0 -100 µM; first doubling time; COLO 858, MEL HO and COLO 679 cells) treatment results in a concentration-dependent cytotoxicity. L-732138 inhibits cell growth with IC50 of 44.6 μM for COLO 858 cells, 76.3 μM for MEL HO cells and 64.2 μM for COLO 679 cells. L-732138 blocks substance P (SP) mitogen stimulation[1].
L-732,138 treatment results in a large number of apoptotic cells were found in COLO 858, MEL HO and COLO 679 melanoma cell lines. In DAPI-stained cultures, at IC50 concentration of 43.6% apoptotic cells for the three melanoma cell lines, whereas at IC100 concentration of 51.4 % apoptotic 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.

Cell Proliferation Assay[1]

Cell Line: COLO 858, MEL HO and COLO 679 cells
Concentration: 0 µM, 20 µM, 40 µM, 60 µM, 80 µM, 100 µM
Incubation Time: First doubling time
Result: Resulted in a concentration-dependent cytotoxicity.

体内研究
(In Vivo)

L-732138 (10-4-10-2 mol/kg; intravenous injection; for 15 minutes; male Dunkin-Hartley guinea-pigs) treatment abolishes vagally-induced plasma exudation and significantly inhibits the enhancement by LPS. The LPS-enhanced vagally-induced plasma exudation is not completely inhibited by either L-732138 or SOD pretreatment alone, but is blocked by the combination of both pretreatments[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.

Animal Model: Male Dunkin-Hartley guinea-pigs (350-500 g) injected with lipopolysaccharide (LPS)[3]
Dosage: 10-4 mol/kg , 10-3 mol/kg and 10-2 mol/kg
Administration: Intravenous injection; for 15 minutes
Result: Abolished the vagally-induced plasma leakage in tracheobronchial tissues, and dose-dependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues.

分子量

472.38

Formula

C22H18F6N2O3
CAS 号

148451-96-1
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 : 250 mg/mL (529.23 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1169 mL 10.5847 mL 21.1694 mL
5 mM 0.4234 mL 2.1169 mL 4.2339 mL
10 mM 0.2117 mL 1.0585 mL 2.1169 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: ≥ 6.25 mg/mL (13.23 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (13.23 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 62.5 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% corn oil

    Solubility: ≥ 6.25 mg/mL (13.23 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (13.23 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 62.5 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]. Muñoz M, et al. The NK-1 Receptor Antagonist L-732,138 Induces Apoptosis and Counteracts Substance P-Related Mitogenesis in Human Melanoma Cell Lines. Cancers (Basel). 2010 Apr 20;2(2):611-23.

    [2]. Cascieri MA, et al. Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor. J Biol Chem. 1994 Mar 4;269(9):6587-91.

    [3]. Kuo HP, et al. Lipopolysaccharide enhances neurogenic plasma exudation in guinea-pig airways. Br J Pharmacol. 1998 Oct;125(4):711-6.

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

可视氮吹仪NK200-1B（样本量：12 孔）

发表于由

【简单介绍】

NK200-1B 可视氮吹仪主要应用于大批量样品的浓缩制备，如药物筛选、激素分析、液相、气相及质谱分析中的样品制备。

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【详细说明】

 

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可视氮吹仪NK200-1B
产品介绍
NK200-1B 可视氮吹仪主要应用于大批量样品的浓缩制备，如药物筛选、激素分析、液相、气相及质谱分析中的样品制备。
    工作原理：通过将氮气吹入加热样品的表面，使样品中的溶剂快速蒸发、分离，从而达到样品无氧浓缩的目的，保持样品更纯净。
    使用氮吹仪代替常用的旋转蒸发仪进行浓缩，能同时浓缩几十个样品，使样品制备时间大为缩短，并且具有省时，易操作，快捷的特点

产品特点
1.加热器使样品被快速有效地加热至蒸发温度,同时气体由气体腔经气针吹至溶液表面,促进溶液快速蒸发和样品浓缩
2.每条吹扫针可独立控制，可以单独进行吹扫，单独进行流量调节，不浪费气体
3.气针在气腔的位置可被改变,使之适用不同的试管.标准气针长度为150mm
4.气腔高度可以调节,本产品具有*的特征：样品浓缩时随时可观察到被浓缩样品的液面位置
5.在浓缩有毒溶剂时,整个系统可置于通风柜中
6.自动故障检测及报警功能
7.标准配备气腔和可调节支架
8.内置超温保护装置
9.即时温度显示、时间递减显示

性能指标
1.温度范围：室温+5℃~150℃
2.升温时间：≤30min （从40℃升至150℃）
3.温度精度@40~100℃：±1℃
4.温度精度@100~150℃：±1.5℃
5.温度稳定性@100：±1℃
6.模块数：1件
7.显示精度:0.1
8.时间设置长:99h59min
9.LED显示
10.氮气流量：0~10L/min
11.氮气压力：≤0.1MPa
12.模块型号选择：参见NK200系列可更换模块

仪器常规配置
1.仪器常规配置：用户可从NK01~NK07规格中任选一规格模块，模块可以互换,常规选NK04或NK05模块
2.大功率400瓦
3.外形尺寸：280x220x500 mm

NK200系列可更换模块

型号
试管直径
试管数
模块尺寸 mm
NK01
 10 mm 
12
153.5 x 96 x 49
NK02
12 mm
12
153.5 x 96 x 49
NK03
13 mm
12
153.5 x 96 x 49
NK04
15 mm
12
153.5 x 96 x 49
NK05
16 mm
12
153.5 x 96 x 49
NK06
19 mm
12
153.5 x 96 x 49
NK07
20 mm
12
153.5 x 96 x 49
 
相关的产品还有：
型号
温度范围
规格
样本量
 NDK200-1
+5 – 150℃
标配 1 个模块
根据选用的模块
 NDK200-2
+5 – 150℃
标配 2 个模块
根据选用的模块
NDK200-1A
+5 – 150℃
标配 1 个模块
根据选用的模块
 NK200-1B
+5 – 150℃
标配 1 个模块
12 孔
 

NK-252

发表于由

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。

NK-252  纯度: 99.93%

NK-252 是一种潜在的 Nrf2 激活剂，具有很好的 Nrf2 活化能力。

NK-252

NK-252 Chemical Structure

CAS No. : 1414963-82-8

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 ￥726 In-stock
5 mg ￥660 In-stock
10 mg ￥1100 In-stock
25 mg ￥2300 In-stock
50 mg ￥4000 In-stock
100 mg ￥6900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

NK-252 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Transcription Factor Targeted Library

生物活性

NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.

IC50 & Target

Nrf2[1]
体外研究
(In Vitro)

The luciferase activity in Huh-7.5 cells treated with Oltipraz (OPZ) or NK-252 shows activation of the NAD(P)H quinone oxidoreductase 1 (NQO1)-ARE in a dose-dependent manner. NK-252 displays this effect with higher potency than OPZ based on the fact that the EC2 value (concentration for a 2-fold induction above background), calculated with linear extrapolation from the values above and below the induction threshold, is 20.8 μM for OPZ and 1.36 μM for NK-252. NK-252 has potential as an Nrf2 activator in hepatic cells. Prototypical Nrf2 activators that include OPZ have been reported to protect microglial cells from H2O2-induced cytotoxicity. The protective effects of OPZ and NK-252 are examined against H2O2-induced cytotoxicity using Huh-7 cells to evaluate their antioxidant properties. The cells treated with OPZ or NK-252 show increased resistance to H2O2-induced cytotoxicity compared with control 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.
体内研究
(In Vivo)

Rats on a choline-deficient L-amino acid–defined (CDAA) diet given OPZ or NK-252 display decreased fibrosis scores compared with CDAA control rats, with median scores of 3, corresponding to bridging fibrosis. CDAA control rats display approximately 20-fold augmentation of the liver fibrosis area compared with rats fed a normal control diet (naive) (14.7 and 0.72%, respectively).This augmentation is also drastically reduced by administration of OPZ or NK-252 (5.80% for OPZ, 6.20% for NK-252_low, and 4.97% for NK-252_high). The effects of NK-252 on both fibrosis score and fibrosis area are dose-dependent[1]. NK-252 alone has no antitumour effect in P388/S- and P388/VCR-mice. The combination therapy of Etoposide with NK-252 administered p.o. significantly increases the life-span of mice inoculated i.p. with P388/S compared with the corresponding therapeutic effects with Etoposide alone. The combination therapy with Etoposide and NK-252 significantly increases the life-span of mice inoculated i.p. with P388/VCR compared with the corresponding survival time with Etoposide alone[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

285.26

Formula

C13H11N5O3
CAS 号

1414963-82-8
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 : ≥ 29 mg/mL (101.66 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 3.5056 mL 17.5279 mL 35.0557 mL
5 mM 0.7011 mL 3.5056 mL 7.0111 mL
10 mM 0.3506 mL 1.7528 mL 3.5056 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: ≥ 2.08 mg/mL (7.29 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.29 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.29 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 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: ≥ 2.08 mg/mL (7.29 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.29 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]. Shimozono R et al. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013 Jul, 84(1):62-70.

    [2]. Kiue A, et al. Enhancement of antitumour activity of etoposide by dihydropyridines on drug-sensitive and drug-resistant leukaemia in mice. Br J Cancer. 1991 Aug;64(2):221-6.
Cell Assay
[1]

The Huh-7.5 cells, a subline derived from Huh-7 cells, are transfected with ARE/pGL4.32 by lipofectamine LTX. The stable clonal transfectant is isolated by selection in hygromycin B (0.1 mg/mL). Cells derived from stable clones are transfected with control or Nrf2 small interfering RNA by lipofectamine RNAiMAX (30 hours), then treated with OPZ, NK-252 (0.1-30 μM, 16 hours) , or DMSO alone (control). The luciferase activity values are measured using the Steady-Glo Luciferase Assay System[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][2]

Rats[1]
Six-week-old male Fischer 344 rats are randomly divided into four compound administration groups and four control groups. Compound administration groups of rats fed a CDAA diet receive oral administration as follows: 1) OPZ from 1 week after feeding at a dose of 60 mg/kg once daily for 9 weeks (CDAA+OPZ group; N=8), 2) NK-252 from 1 week after feeding at a dose of 20 mg/kg once daily for 9 weeks (CDAA+NK-252_low group; N=8), 3) NK-252 from 1 week after feeding at a dose of 60 mg/kg once daily for 9 weeks (CDAA+NK-252_high group; N=8), or 4) NK-252 from 6 weeks after feeding at a dose of 60 mg/kg once daily for 4 weeks (CDAA+NK-252_delayed administration: DA group; N=7). Two control groups of rats are fed a CDAA diet for 6 or 10 weeks (pre-CDAA control or CDAA control group; N=9 each), and the other two control groups of rats are fed standard rodent chow (CRF-1) for 6 or 10 weeks (prenaive or naive; N=3 each). Laparotomy and blood sampling are performed under isoflurane anesthesia. After blood sampling, rats are euthanized by exsanguination under isoflurane anesthesia, and the livers are immediately extirpated. [2]Mice[2]
Six- to 8-week-old male BALB/c x DBA/2 F1 (hereafter called CD2F1) mice weighing 22 to 26 g are used. Male CD2F1 mice are inoculated i.p. with 106 cells of P388/S and P388/VCR cell line on day 0. Each group consist of six mice. NK-250 and NK-252 (100, 300, and 1000 mg/kg) are given p.o. daily from day 1 to 5. Mean survival days and the range of survival days are analysed.

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]. Shimozono R et al. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013 Jul, 84(1):62-70.

    [2]. Kiue A, et al. Enhancement of antitumour activity of etoposide by dihydropyridines on drug-sensitive and drug-resistant leukaemia in mice. Br J Cancer. 1991 Aug;64(2):221-6.

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