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/ HIF / Oltipraz/奥替普拉

Oltipraz/奥替普拉 {[allProObj[0].p_purity_real_show]}

货号：A169991 同义名： 吡噻硫酮 / RP 35972; NSC 347901

Oltipraz can inhibit the insulin-activated HIF-1α (IC50 = 10 µM) in a time-dependent manner.

Oltipraz/奥替普拉 化学结构 CAS号：64224-21-1
Oltipraz/奥替普拉 化学结构
CAS号：64224-21-1
Oltipraz/奥替普拉 3D分子结构
CAS号：64224-21-1
Oltipraz/奥替普拉 化学结构 CAS号：64224-21-1
Oltipraz/奥替普拉 3D分子结构 CAS号：64224-21-1
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Oltipraz/奥替普拉 纯度/质量文件 产品仅供科研

货号：A169991 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 HIF ↓ HIF1 ↓ PHD1 ↓ PHD2 ↓ PHD3 ↓ 其他靶点 纯度
KC7F2 +

HIF-1α, IC50: 20 μM

 		+

HIF-1α, IC50: 20 μM

 		98%
Lificiguat ✔ 99%+
BAY 87-2243 ✔ 99%+
PX-478·2HCl ✔ 98%+
2-Methoxyestradiol ✔ 98%
CAY10585 ++

HIF, IC50: 4.4 μM

 		BCRP 97%
DMOG ✔ 98%
FG 2216 ++

PHD2, IC50: 3.9 μM

 		99%+
MK-8617 ++++

PHD1, IC50: 1 nM

 		++++

PHD2, IC50: 1 nM

 		++++

PHD3, IC50: 14 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Oltipraz/奥替普拉 生物活性

描述 Oltipraz is a potent chemopreventive agent which can inhibit the carcinogenicity of many environmental carcinogens in multiple target organs[6]. It is regarded as an activator of Nrf2. Treatment with Oltipraz led increased nuclear Nrf2 protein in liver sections from Oltipraz -treated mice. Also it led an induction of hepatic Mrp transporters through the Nrf2 transcriptional pathway[7]. Oltipraz coordinately increases multiple hepatic xenobiotic transporter mRNA levels. Sprague-Dawley rats treated with OPZ exhibited CAR-dependent increased mRNA and protein levels of both Nqo1 and Cyp2b1/2 by 24 h. But it induced microsomal epoxide hydrolase, NAD(P)H quinone oxidoreductase, and Cyp3a1/23, independent of CAR[8].

Oltipraz/奥替普拉 动物研究

Dose Rat: 10 mg/kg[4] (i.v.), 5 mg/kg - 20 mg/kg[5] (i.v.); 30 mg/kg[4] (p.o.), 25 mg/kg - 100 mg/kg[5] (p.o.) Mice: 5 mg/kg - 20 mg/kg[5] (i.v.); 15 mg/kg - 50 mg/kg[5] (p.o.)
Administration i.v., p.o.
Pharmacokinetics
Animal Rats[4]
Dose 10 mg/kg (i.v.)
30 mg/kg (p.o.)
Administration i.v.
p.o.
MRT 61.5 ± 15.6 h (i.v.)
F 30.3% (p.o.)
T1/2 76.5 ± 18.2 h (i.v.)
129 ± 54.6 h (p.o.)
Tmax 390 ± 239 h (p.o.)
Cmax 0.286 ± 0.0929 μg/ml (p.o.)
Vss 4120 ± 1490 ml/kg (i.v.)
AUC 155 ± 26.7 μg·min/ml (i.v.)
141 ± 28.8 μg·min/ml (p.o.)

Oltipraz/奥替普拉 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01393678 Chronic Liver Disease Phase 3 Completed - Korea, Republic of ... 展开 >> Hanyang University Hospital Seoul, Seongdong-gu,, Korea, Republic of 收起 <<
NCT00006457 Lung Cancer Phase 1 Completed - United States, Illinois ... 展开 >> Robert H. Lurie Comprehensive Cancer Center, Northwestern University Chicago, Illinois, United States, 60611-3013 United States, North Carolina Duke Comprehensive Cancer Center Durham, North Carolina, United States, 27710 收起 <<
NCT01373554 Non-alcoholic Fatty Liver Dise... 展开 >>ase 收起 << Phase 2 Completed - Korea, Republic of ... 展开 >> Inje University Ilsan Paik Hospital Dahwa-dong, Ilsanseo-gu, Goyang-si, Gyeonggi-do, Korea, Republic of, 411-706 NHUS Ilsan Hospital Ilsan-ro Ilsan-donggu, Goyang-si, Korea, Republic of, 410-719 Seoul National University Hospital Daehak-ro Jongno-gu, Seoul, Korea, Republic of, 110-744 Korea University Guro hospital Gurodong-ro, Seoul, Korea, Republic of, 152-703 Boramae Hospital Sindaebang-dong Dongjak-gu, Seoul, Korea, Republic of, 156-707 收起 <<

Oltipraz/奥替普拉 参考文献

[1]Manandhar S, Cho JM, et al. Induction of Nrf2-regulated genes by 3H-1, 2-dithiole-3-thione through the ERK signaling pathway in murine keratinocytes. Eur J Pharmacol. 2007 Dec 22;577(1-3):17-27. Epub 2007 Aug 23.

[2]Maher JM, Dieter MZ, et al. Oxidative and electrophilic stress induces multidrug resistance-associated protein transporters via the nuclear factor-E2-related factor-2 transcriptional pathway. Hepatology. 2007 Nov;46(5):1597-610.

[3]Merrell MD, Augustine LM, et al. Induction of drug metabolism enzymes and transporters by oltipraz in rats. J Biochem Mol Toxicol. 2008 Mar-Apr;22(2):128-35.

[4]Lee DY, Kim JW, et al. Pharmacokinetic interaction between oltipraz and omeprazole in rats: Competitive inhibition of metabolism of oltipraz by omeprazole via CYP1A1 and 3A2, and of omeprazole by oltipraz via CYP1A1/2, 2D1/2, and 3A1/2. Eur J Pharm Sci. 2007 Dec;32(4-5):328-39. Epub 2007 Aug 31.

[5]Bae SK, Lee SJ, et al. Interspecies pharmacokinetic scaling of oltipraz in mice, rats, rabbits and dogs, and prediction of human pharmacokinetics. Biopharm Drug Dispos. 2005 Apr;26(3):99-115.

[6]Manandhar S, Cho JM, Kim JA, Kensler TW, Kwak MK. Induction of Nrf2-regulated genes by 3H-1, 2-dithiole-3-thione through the ERK signaling pathway in murine keratinocytes. Eur J Pharmacol. 2007 Dec 22;577(1-3):17-27. doi: 10.1016/j.ejphar.2007.08.018. Epub 2007 Aug 23. PMID: 17854798.

[7]Maher JM, Dieter MZ, Aleksunes LM, Slitt AL, Guo G, Tanaka Y, Scheffer GL, Chan JY, Manautou JE, Chen Y, Dalton TP, Yamamoto M, Klaassen CD. Oxidative and electrophilic stress induces multidrug resistance-associated protein transporters via the nuclear factor-E2-related factor-2 transcriptional pathway. Hepatology. 2007 Nov;46(5):1597-610. doi: 10.1002/hep.21831. PMID: 17668877.

[8]Merrell MD, Augustine LM, Slitt AL, Cherrington NJ. Induction of drug metabolism enzymes and transporters by oltipraz in rats. J Biochem Mol Toxicol. 2008 Mar-Apr;22(2):128-35. doi: 10.1002/jbt.20225. PMID: 18418891.

Oltipraz/奥替普拉 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.42mL

0.88mL

0.44mL

22.09mL

4.42mL

2.21mL

44.18mL

8.84mL

4.42mL

Oltipraz/奥替普拉 技术信息

CAS号64224-21-1
分子式C8H6N2S3
分子量 226.34
SMILES Code S=C1SSC(C2=NC=CN=C2)=C1C
MDL No. MFCD00868499
别名 吡噻硫酮 ;RP 35972; NSC 347901; CD1400
运输蓝冰
InChI Key CKNAQFVBEHDJQV-UHFFFAOYSA-N
Pubchem ID 47318
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

Tags: Oltipraz | RP 35972;NSC 347901;CD1400 | 吡噻硫酮 | HIF | AmBeed-信号通路专用抑制剂 | Oltipraz/奥替普拉 纯度/质量文件 | Oltipraz/奥替普拉 亚型比较 | Oltipraz/奥替普拉 生物活性 | Oltipraz/奥替普拉 动物研究 | Oltipraz/奥替普拉 临床数据 | Oltipraz/奥替普拉 参考文献 | Oltipraz/奥替普拉 实验方案 | Oltipraz/奥替普拉 技术信息

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