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PF-04981517
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产品介绍
产品信息
简单描述
A potent, selective inhibitor of CYP3A4
商品描述
PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM).1 It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively).1 PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.
分子量
456.6
纯度
≥98%
背景
别名
CYP3cide
结构式
CC1=CC=C(C2=C(C3=NN(C)C4=C3C(N5C[C@@H](N6CCCCC6)CC5)=NC=N4)C=NN2C)C=C1
分子式
C26H32N8
CAS号
1390637-82-7
制备和贮存
保存
≥ 4 years
溶解方法
DMF: 30 mg/ml
DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml
DMSO: 20 mg/ml
Ethanol: 2 mg/ml
保存方式
-20°C
文献
文献
1.Bibi, Z. Role of cytochrome P450 in drug interactions. Nutrition & Metabolism 5(27), 1-10 (2008).
2.Walsky, R.L.,Obach, R.S.,Hyland, R., et al. Selective mechanism-based inactivation of cytochrome P4503A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of cytochrome P4503A4 versus P4503A5 in the metabolism of drugs. Drug Metabolism and Disposition 40(9), 1686-1697 (2012).
2.Walsky, R.L.,Obach, R.S.,Hyland, R., et al. Selective mechanism-based inactivation of cytochrome P4503A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of cytochrome P4503A4 versus P4503A5 in the metabolism of drugs. Drug Metabolism and Disposition 40(9), 1686-1697 (2012).
参考图片
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