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4-phenyl-5-methyl-1,2,3-Thiadiazole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
4-phenyl-5-methyl-1,2,3-Thiadiazole图片
CAS NO:64273-28-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1g电议
5g电议

产品介绍
Cas No.64273-28-5
别名5-甲基-4-苯基-1,2,3-噻二唑,NSC 358739
化学名5-methyl-4-phenyl-1,2,3-thiadiazole
Canonical SMILESCc1snnc1c1ccccc1
分子式C9H8N2S
分子量176.2
溶解度≥ 7.85mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

4-phenyl-5-methyl-1,2,3-Thiadiazole is a CYP2B4 and CYP2E1 inhibitor.

Cytochrome P450 (CYP450) enzymes, a superfamily of oxidative catalysts, are important in the biosynthesis and metabolism of a wide range of endogenous molecules and the metabolism of xenobiotics. CYP2B4 can metabolize substituted amines, while CYP2E1 metabolizes various alcohols and halogenated alkenes.

In vitro: 4-phenyl-5-methyl-1,2,3-Thiadiazole (PMT) was found to be slightly more inhibitory to P450s 2E1 and 1A2 than its close analog, 4,5-diphenyl-1,2,3-thiadiazole (DPT). By contrast, 4-phenyl-5-hydrogen-1,2,3-Thiadiazole (PT), a weaker inhibitor than DPT and PMT with P450s 2E1 and 2B4, was comparable to PMT and more effective than DPT with P450 1A2. Moreover, PMT, DPT, as well as PT showed no inactivation of either P450 2E1 or 2B4, though they were fairly effective inhibitors, and the thiadiazole ring could be oxidized by the P450 system. Furthremore, the lack of inactivation of the P450 isoforms by PMT, DPT, and PT suggested that a transient reactive intermediate was not formed on oxidation of the thiadiazole ring. In additioin, the 1,2,3-thiadiazole ring could be oxidized by the P450 system [1].

In vivo: Up to now, there is no animla in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Babu, B. R. and Vaz, A.D.N. 1,2,3-thiadiazole: A novel heterocyclic heme ligand for the design of cytochrome P450 inhibitors. Biochemistry 36, 7209-7216 (1997).