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