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Evacetrapib

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Chemical Structure| 1186486-62-3 同义名 : LY2484595
CAS号 : 1186486-62-3
货号 : A293328
分子式 : C31H36F6N6O2
纯度 : 98%
分子量 : 638.647
MDL号 : MFCD23105886
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(164.41 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

15% Captisol+water 30 mg/mL suspension

生物活性
靶点

  • CETP

    CETP, IC50:5.5 nM
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.83mL

1.57mL

0.78mL

15.66mL

3.13mL

1.57mL
参考文献

[1]Aronow WS. Effect of evacetrapib on cardiovascular outcomes in patients with high-risk cardiovascular disease. J Thorac Dis. 2017 Jul;9(7):1822-1825.

[2]Cao G, Beyer TP, et al. 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.

[3]Cao G, Beyer TP, Zhang Y, et al. 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;52(12):2169-2176. doi:10.1194/jlr.M018069