CAS:1186486-62-3Evacetrapib

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Synonyms: LY-2484595

Evacetrapib is a potent and selective inhibitor of CETP with IC50 of 5.5 nM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1186486-62-3

储存条件

分子式

C31H36F6N6O2

运输

蓝冰

分子量

638.65

别名

LY-2484595

溶解度

动物实验配方

15% Captisol+water

30 mg/mL

suspension

生物活性

描述Cholesteryl ester transfer protein (CETP) is a glycoprotein that catalyzes the reciprocal neutral lipid exchange between HDL and apoB-containing lipoprotein particles. Evacetrapib is a potent and selective inhibitor of CETP that inhibits human recombinant CETP protein with an IC50 of 5.5nM and inhibits CETP activity in human plasma in vitro with an IC50 value of 26nM. In human ApoAI and CETP double transgenic mice, oral administration of evacetrapib at 30mg/kg resulted in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4, 8 and 24h, respectively, after treatment. Evacetrapib at 1-30mg/kg dose-dependently inhibited CETP activity in vivo at 8h post-treatment. Treatment with evacetrapib (10 and 30mg/kg) also elevated the level of HDL-C in these animals.^[3]
作用机制Evacetrapib is a novel benzazepine-based CETP inhibitor that inhibits CETP activity both in vitro and in vivo without increasing blood pressure or inducing synthesis of aldosterone or cortisol.^[3]