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Oltipraz

Oltipraz

产品编号 T0153   CAS 64224-21-1
别名: 吡噻硫酮, NSC 347901, RP 35972

Oltipraz (RP 35972) 是一种 Nrf2的强效激活剂。它时间依赖性地抑制 HIF-1α激活,IC50为 10 μM,浓度 ≥ 10 μM 时完全消除 HIF-1α诱导。

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Oltipraz Chemical Structure
Oltipraz, CAS 64224-21-1
规格 价格/CNY 货期 数量
5 mg ¥ 255 现货
10 mg ¥ 418 现货
25 mg ¥ 614 现货
50 mg ¥ 756 现货
100 mg ¥ 1,178 现货
200 mg ¥ 1,516 现货
500 mg ¥ 2,192 现货
1 mL * 10 mM (in DMSO) ¥ 460 现货
产品目录号及名称: Oltipraz (T0153)
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纯度: 100%
纯度: 99.56%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.
靶点活性 HIF-1α:10 μM
体外活性 Oltipraz, as a chemoprotective agent, induces Phase II detoxification enzyme activity in a Nrf2-dependent manner. [1] In human HT29 colon cancer cells, oltipraz inhibits the induction of HIF-1α by insulin, hypoxia or CoCl2 by significantly accelerating degradation of HIF-1α protein. [2]
体内活性 Oltipraz (500 mg/kg, p.o.) significantly reduces multiplicity of gastric neoplasia in wild-type mice by 55%, but has no effect on tumor burden in nrf2-deficient mice. [1] In BALB/c nude mice transplanted with HCT116 cells, Oltipraz (200 mg/kg, p.o.) inhibits tumor growth and angiogenesis via inhibition of HIF-1α. [2] In rats on a CDAA diet, Oltipraz attenuate the progression of nonalcoholic steatohepatitis-related fibrosis. [3]
激酶实验 The Src and Abl kinase assays: The Src kinase activity is measured in an ELISA format. Src (3 units/reaction), reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4) and cdc2 substrate peptide are added to various concentration of Bosutinib and incubated at 30 °C for 10 minutes. The reaction is started by the addition of ATP to a final concentration of 100 μM, incubated at 30 °C for 1 hour and stopped by addition of EDTA. Instructions from the manufacturer are followed for subsequent steps. The Abl kinase assay is performed in a DELFIA solid phase europium-based detection assay format. Biotinylated peptide (2 μM) is bound to streptavidin-coated microtitration plates for 1.5 hours in 1 mg/mL ovalbumin in PBS. The plates are washed for 1 hour with PBS/0.1% Tween 80, followed by a PBS wash. The kinase reaction is incubated for 1 hour at 30°C. Abl kinase (10 units) is mixed with 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4, 1% DMSO, 1 mM HEPES (pH 7.0), 200 μg/mL ovalbumin and various concentration of Bosutinib. The reaction is stopped with EDTA at a final concentration of 50 mM. The reaction is monitored with Eu-labeled phosphotyrosine antibody and DELFIA enhancement solution.
别名 吡噻硫酮, NSC 347901, RP 35972
分子量 226.34
分子式 C8H6N2S3
CAS No. 64224-21-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 11.3 mg/mL (50 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.4181 mL 22.0907 mL 44.1813 mL 110.4533 mL
5 mM 0.8836 mL 4.4181 mL 8.8363 mL 22.0907 mL
10 mM 0.4418 mL 2.2091 mL 4.4181 mL 11.0453 mL
20 mM 0.2209 mL 1.1045 mL 2.2091 mL 5.5227 mL
50 mM 0.0884 mL 0.4418 mL 0.8836 mL 2.2091 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Ramos-Gomez M, et al. Proc Natl Acad Sci U S A. 2001, 98(6), 3410-3415.. 2. Lee WH, et al. Mol Cancer Ther. 2009, 8(10), 2791-2802. 3. Shimozono R, et al. Mol Pharmacol. 2013, 84(1), 62-70.
AT 14 acetate Coniferaldehyde Gingerenone A 4-hydroxyphenylacetic acid ML334 Rehmapicrogenin Moringin Garcinone D

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌活性化合物库 神经退行性疾病化合物库 抗癌临床化合物库 免疫/炎症分子化合物库 抗胰腺癌化合物库 抗阿尔茨海默症化合物库 抗感染化合物库 经典已知活性库 人代谢物化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Oltipraz 64224-21-1 Angiogenesis Chromatin/Epigenetic Immunology/Inflammation Metabolism Microbiology/Virology Proteases/Proteasome HIF HIV Protease Reverse Transcriptase HIF/HIF Prolyl-Hydroxylase Nrf2 Inhibitor Keap1-Nrf2 RP35972 inhibit HIFs Human immunodeficiency virus HIV Hypoxia-inducible factors 吡噻硫酮 NSC347901 NSC-347901 RP-35972 NSC 347901 RP 35972 HIF-PH inhibitor

 

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