CYP3cide (PF-4981517) 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 Midazolam 1'-羟化酶活性的IC50值分别为 0.03 μM，17 μM 和 71μM。CYP3cide 可用于区分CYP3A4和 CYP3A5 对于药物代谢的作用。

CYP3cide (PF-4981517) is a efficient, specific and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC 50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide is able to be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug metabolism [1].

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 midazolam 1'-hydroxylase activity to CYP3A5 abundance is significant [1].

1390637-82-7

C26H32N8

456.59

CYP3cide

DMSO:9mg/mL (19.7mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years