| 货号 | 14844-5g |
| 描述 | CYP2C9 is a major cytochrome P450 enzyme that is involved in the metabolic clearance of various therapeutic agents. Disruption of this enzyme’s activity can lead to adverse drug reactions.1 Sulfaphenazole is an inhibitor of CYP2C9 (Ki = 0.3 μM) that demonstrates at least 100-fold selectivity over other CYP450 isoforms (Kis = 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).2,3 At 10 μM, sulfaphenazole has been shown to inhibit endothelium-derived hyperpolarizing factor synthase, a CYP450 isozyme in the porcine coronary artery homologous to CYP2C8/9 that generates reactive oxygen species in coronary endothelial cells and modulates vascular tone and homeostasis.4 |
| 别名 | Depocid;Depotsulfonamide;Plisulfan;Raziosulfa; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Rettie, A.E. and Jones, J.P. Clinical and toxicological relevance of CYP2C9: Drug-drug interactions and pharmacogenetics. Annual Reviews of Pharmacology and Toxicology 45, 477-494 (2005). 2.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. Biochemistry 35(50), 16205-16212 (1996). 3.Sai, Y.,Dai, R.,Yang, T.J., et al. Assessment of specificity of eight chemical inhibitors using cDNA-expressed cytochromes P450. Xenobiotica 30(4), 327-343 (2000). 4.Fleming, I.,Michaelis, U.R.,Bredenkötter, D., et al. Endothelium-derived hyperpolarizing factor synthase (cytochrome P450 2C9) is a functionally significant source of reactive oxygen species in coronary arteries. Circulation Research 88(1), 44-51 (2001). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 314.4 |
| 分子式 | C15H14N4O2S |
| CAS号 | 526-08-9 |
| 稳定性 | ≥ 2 years |
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