CAS:64224-21-1Oltipraz

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Oltipraz 吡噻硫酮 Cat No. FB07835Cas No. 64224-21-1

Synonyms: RP-35972;NSC-347901

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

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.4181 mL
- 22.0905 mL
- 44.1810 mL
- 5 mM
- 0.8836 mL
- 4.4181 mL
- 8.8362 mL
- 10 mM
- 0.4418 mL
- 2.2091 mL
- 4.4181 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

64224-21-1

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C8H6N2S3

运输

蓝冰

分子量

226.34

别名

RP-35972;NSC-347901

溶解度

DMSO	58.33 mg/mL (257.7 mM) warming
Water	insoluble

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

靶点数据

生物活性

靶点 HIF1α

IC50:10μM
描述Oltipraz is a potent chemopreventive agent which can inhibit the carcinogenicity of many environmental carcinogens in multiple target organs. 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. 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.

动物研究

剂量

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.)

给药途径

i.v., p.o.

动物药代数据

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.)
T_1/2	76.5 ± 18.2 h (i.v.) 129 ± 54.6 h (p.o.)
T_max	390 ± 239 h (p.o.)
C_max	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.)