化合物PF-4981517 T21548

Product Introduction
Bioactivity


英文名: PF-4981517

描述: PF-4981517 (CYP3cide) 是一种高效，特异性和时间依赖性细胞色素P4503A4 (CYP3A4)抑制剂。对于CYP3A4，CYP3A5 和 CYP3A7，抑制CYP3A 活性的IC50值分别为 0.03 μM，17 μM 和 71μM。PF-4981517 可用于区分CYP3A4和 CYP3A5 对于药物代谢的作用。

体外活性: When investigating the inhibition of CYP3cide, an extreme metabolic inactivation efficiency (k inact /K I ) of 3300 to 3800 ml min -1 μmol -1 is observed in human liver microsomes from donors of nonfunctioning CYP3A5 (CYP3A5 * 3/ * 3). This observed efficiency equated to an apparent KI between 420 and 480 nM with a maximal inactivation rate (kinact) equal to 1.6 min -1. When CYP3cide is tested at a concentration and preincubation time to completely inhibit CYP3A4 in a library of genotyped polymorphic CYP3A5 microsomes, the correlation of the remaining CYP3A activity to CYP3A5 abundance is significant.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 9 mg/mL (19.7 mM)


关键字: PF 4981517 | PF-4981517 | PF4981517

相关产品: Canadine | Pisatin | 8alpha-(2-Methylacryloyloxy)hirsutinolide 13-O-acetate | Schizandrin A | Furafylline | CAY10434 | Oteseconazole | Fomepizole | Uniconazole | Diflubenzuron

相关库: Anti-Cancer Compound Library | Anti-Metabolism Disease Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Highly Selective Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途