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Sulfaphenazole
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。
Sulfaphenazole图片
CAS NO:526-08-9
规格:98%
分子量:314.4
包装与价格:
包装价格(元)
250mg电议
500mg电议
1g电议
5g电议

产品介绍
CYP2C9 inhibitor
CAS:526-08-9
分子式:C15H14N4O2S
分子量:314.4
纯度:98%
存储:Store at -20°C

Background:

Sulfaphenazole is a strong and competitive inhibitor of CYP2C9 [1]. CYP2C9 is a major cytochrome P450 enzyme involved in the metabolic clearance of various therapeutic agents, such as oral anticoagulants, nonsteroidal anti-inflammatories, and oral hypoglycemics. Disruption of CYP2C9 activity results in many adverse drug reactions [2].


In vitro: In yeast expressed human cytochromes P450 of the 1A, 3A, and 2C subfamilies, sulfaphenazole acts as a strong and competitive inhibitor of CYP 2C9 with the Ki value of 0.3 ± 0.1 μM. The Ki values of sulfaphenazole for CYP 2C8 and 2C18 were 63 and 29 μM, respectively. Sulfaphenazole failed to inhibit CYP 1A1, 1A2, 3A4, and 2C19 [1].


In vivo: In diabetic male mice (db/db strain), daily intraperitoneal injections of either the CYP 2C inhibitor sulfaphenazole (5.13 mg/kg) for 8 weeks, sulfaphenazole restored endothelium-mediated relaxation in db/db mice. Sulfaphenazole reduced oxidative stress, increased NO bioavailability and restored endothelial function in db/db mice [3].


参考文献:
[1] Mancy A, Dijols S, Poli S, et al.  Interaction of sulfaphenazole derivatives with human liver cytochromes P450 2C: molecular origin of the specific inhibitory effects of sulfaphenazole on CYP 2C9 and consequences for the substrate binding site topology of CYP 2C9[J]. Biochemistry, 1996, 35(50): 16205-16212.
[2] Rettie A E, Jones J P.  Clinical and toxicological relevance of CYP2C9: drug-drug interactions and pharmacogenetics[J]. Annu. Rev. Pharmacol. Toxicol., 2005, 45: 477-494.
[3] Elmi S, Sallam N A, Rahman M M, et al.  Sulfaphenazole treatment restores endothelium-dependent vasodilation in diabetic mice[J]. Vascular pharmacology, 2008, 48(1): 1-8.