PF-4981517

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CYP3cide (PF-4981517) 是一种有效，选择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 在活性分子代谢中的作用。

CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on agent metabolism.

When investigating the inhibitory properties of CYP3cide, an extreme metabolic inactivation efficiency (kinact/KI) of 3300 to 3800 ml ? min-1 ? μmol-1 is observed using 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.

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Metabolic Enzyme/Protease

P450

P450

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1390637-82-7

456.59

C26H32N8

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (109.51 mM; 超声助溶 (<60°C)

Cc1ccc(cc1)-c1c(cnn1C)-c1nn(C)c2ncnc(N3CC[C@@H](C3)N3CCCCC3)c12

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(-20℃)

With Ice Pack

≥ 2 years