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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)
50mg电议
100mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt200.2
Cas No.152467-47-5
FormulaC6H4N2O2S2
SynonymsMTCC
Solubility≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical Namemethylthieno[3,2-d][1,2,3]thiadiazole-6-carboxylate
Canonical SMILESO=C(OC)C1=CSC2=C1N=NS2
运输条件蓝冰运输或根据您的需求运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

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).