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Evacetrapib(LY2484595)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Evacetrapib(LY2484595)图片
CAS NO:1186486-62-3
规格:98%
分子量:638.65
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
200mg电议

产品介绍
CETP inhibitor,potent and selective
CAS:1186486-62-3
分子式:C31H36F6N6O2
分子量:638.65
纯度:98%
存储:Store at -20°C

Background:

Evacetrapib is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) with IC50 value of 5.5nM [1].


As a benzazepine-based inhibitor of CETP, evacetrapib is developed to increase HDL cholesterol for the treatment of coronary artery disease. Evacetrapib is efficacious both in vitro and in vivo. The IC50 values of evacetrapib against CETP are 5.5nM and 26nM, respectively in the buffer assay using human recombinant CETP and in the plasma assay using human plasma CETP. In the animal model of human CETP/ApoAI double transgenic mouse line, oral administration of evacetrapib at 30mg/kg significantly inhibits the CETP activity as well as increases the level of HDL. Besides that, the ED50 value of evacetrapib is less than 5mg/kg. Compared to the previous inhibitors of CETP, evacetrapib has less side effects. It is found no to increase blood pressure Zucker diabetic fatty rats and not to induce aldosterone or cortisol synthesis in H295R cells [1].


参考文献:
[1] Cao G, Beyer TP, Zhang Y, Schmidt RJ, Chen YQ, Cockerham SL, Zimmerman KM, Karathanasis SK, Cannady EA, Fields T, Mantlo NB. Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure. J Lipid Res. 2011 Dec;52(12):2169-76.