Oltipraz|64224-21-1|(奥替普拉; RP 35972; NSC 347901)-陌孚医药/Medlife

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Oltipraz (Synonyms: 奥替普拉; RP 35972; NSC 347901)

目录号: PL02741 纯度: ≥99%

CAS No. :64224-21-1

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中文名称	Oltipraz
中文别名	吡噻硫酮;2-乙基苯甲醛;奥替普拉-D3;奥替普拉
英文名称	Oltipraz
英文别名	3H-1,2-Dithiole-3-thione,4-methyl-5-(2-pyrazinyl)-;Oltipraz;4-Methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione;4-methyl-5-pyrazin-2-yldithiole-3-thione;3H-1,2-DITHIOLE-3-THIONE,4-METHYL-5-PYRAZINYL;4-Methyl-5-pyrazin-2-yl-1,2-dithiole-3-thione;4-Methyl-5-pyrazinyl-3H-1,2-dithiole-3-thione;NSC 347901;RP 35972;RP-35,972;4-Methyl-5-(2-pyrazinyl)-1,2-dithiole-3-thione;BRN 0978110;CCRIS 4048;Oltiprazum;Oltipraz [INN];Oltiprazum [INN-Latin];3H-1,2-DITHIOLE-3-THIONE, 4-METHYL-5-PYRAZINYL-;5-(2-Pyrazinyl)-4-methyl-1,2-dithiole-3-thione;C8H6N2S3;6N510JUL1Y;4-Methyl-5-(pyrazinyl)-3H-1,2-dithiole-3-thione;NSC347901;AK1
Cas No.	64224-21-1
分子式	C₈H₆N₂S₃
分子量	226.34
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Oltipraz 抑制 HIF-1α 激活, 这种作用具时间依赖性, 浓度 ≥ 10 μM 时完全消除 HIF-1α 诱导, Oltipraz 抑制 HIF-1α, IC₅₀ 为 10 μM。Oltipraz 还是一种强效的 Nrf2 激活剂。

生物活性

Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC 50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.

性状

Solid

IC50 & Target[1][2]

IC50: 10 μM (HIF-1α);
Nrf2

体外研究(In Vitro)

Oltipraz inhibits HIF-1α activity and HIF-1α-dependent tumor growth, which may result from a decrease in HIF-1α stability through S6K1 inhibition in combination with an H2O2-scavenging effect. Oltipraz treatment also inhibits HIF-1α activation stimulated by either hypoxia or CoCl2. Oltipraz is a cancer chemopreventive agent and has an inhibitory effect on angiogenesis and tumor growth. [1] Oltipraz is also a competitive inhibitor of this cytochrome P450, with an apparent Ki of 10 μM. [2] has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In wild-type mice, hepatic levels of mRNA for all of the genes analyzed were significantly increased after Oltipraz treatment, with the highest increase (treated/control) for NQO1 mRNA levels (7.6-fold). The Northern blot analyses demonstrated that the observed increases in GST and NQO1 activities by Oltipraz in wild-type mice were preceded by significant elevations in RNA expression. Interestingly, mRNA levels of Nrf2 itself were increased more than 3-fold by Oltipraz treatment. [2] has not independently confirmed the accuracy of these methods. They are for reference only.

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

ClinicalTrial

参考文献

[1]. Lee WH, et al. Oltipraz and dithiolethione congeners inhibit hypoxia-inducible factor-1alpha activity through p70 ribosomal S6 kinase-1 inhibition and H2O2-scavenging effect. Mol Cancer Ther. 2009 Oct;8(10):2791-802.
[2]. Lv S, et al. Glucagon-induced extracellular cAMP regulates hepatic lipid metabolism. J Endocrinol. 2017 Aug;234(2):73-87.

溶解度数据	In Vitro: DMSO : 6 mg/mL (26.51 mM; Need ultrasonic and warming)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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