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2,3-dihydrothieno-Thiadiazole Carboxylate
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。
2,3-dihydrothieno-Thiadiazole Carboxylate图片
CAS NO:152467-47-5
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议

产品介绍
CYP450 enzymes (CYP2E1 and CYP2B4) inhibitor
Cas No.152467-47-5
别名MTCC
化学名methylthieno[3,2-d][1,2,3]thiadiazole-6-carboxylate
Canonical SMILESO=C(OC)C1=CSC2=C1N=NS2
分子式C6H4N2O2S2
分子量200.2
溶解度≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
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

2,3-dihydrothieno-Thiadiazole Carboxylate is a CYP450 (CYP2E1 and CYP2B4) inhibitor.

The cytochrome P450 (CYP) enzymes are a superfamily of oxidative catalysts critical in the biosynthesis and metabolism of various endobiotics such as steroids and steroid hormones, the neurotransmitter nitric oxide, and vitamins A and D. The cytochrome P450 enzymes are also involved in the metabolism of xenobiotics including natural products, drugs, and other organic chemicals.

In vitro: As a 1,2,3-thiadiazole analog, 2,3-dihydrothieno-thiadiazole carboxylate could both inhibit and inactivate certain microsomal CYP450 enzymes (CYP2E1 and CYP2B4) at 100 μM, but not others (CYP1A2). Moreover, P450 2E1 was significantly more sensitive than P450 2B4 to mechanism-based inactivation by 2,3-dihydrothieno-thiadiazole carboxylate when compared by the difference in partition numbers and inactivation rate constants. Inactivation rate constants (kinact) determined from plots of 1/kobs versus 1/[I] were 0.08 for 2E1 and 0.04 min-1 for P450 2B4, with Kis of 0.1 and 2.0 mM, respectively. The difference in the oxidation of the monocyclic and bicyclic thaidiazoles might account for the ability of 2,3-dihydrothieno-thiadiazole carboxylate to function as a mechanism-based inactivator [1].

In vivo: Up to now, there is no animal 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).