Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 11.3 mg/mL (50 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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