CAS NO: | 152467-47-5 |
包装 | 价格(元) |
50mg | 电议 |
100mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 200.2 |
Cas No. | 152467-47-5 |
Formula | C6H4N2O2S2 |
Synonyms | MTCC |
Solubility | ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | methylthieno[3,2-d][1,2,3]thiadiazole-6-carboxylate |
Canonical SMILES | O=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。 |
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).