产品描述
| 溶解性 |
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| 存贮条件 | 储存温度-20°C |
| 产品介绍 |
Evacetrapib (LY2484595)是高活性CETP选择性抑制剂，IC50为5.5 nM，能在不增加醛固酮和血压的情况下提高高密度脂蛋白胆固醇。 |
| 生化机理 |
Evacetrapib (LY2484595) inhibits human plasma CETP protein with IC50 of 26 nM. Evacetrapib (LY2484595) (< 10 μM) does not induce aldosterone or cortisol synthesis in H295R cells. Evacetrapib (LY2484595) (30 mg/kg, orally) results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4 hours, 8 hours and 24 hours post dose respectively in human ApoAI and CETP double transgenic mice. Evacetrapib (LY2484595) (30 mg/kg) results in 129.7% increase in HDL-C 8 hours after oral administration. The ED50 values of CETP inhibitory activity 8 hours post oral dosing for Evacetrapib (LY2484595) in two dose-response studies are calculated to be 3.5 mg/kg and 4.1 mg/kg respectively. Evacetrapib (LY2484595) (< 200 mg/kg) does not increase blood pressure in Zucker diabetic fatty rats. |
| 别名 | LY2484595;LY 2484595;LY-2484595;反式-4-(((5S)-5-(((3,5-双(三氟甲基)苯基)甲基)(2-甲基-2H-四氮唑-5-基)氨基)-2,3,4,5-四氢-7,9-二甲基-1H-1-苯并氮杂卓-1-基)甲基)环己烷羧酸;;LY2484595;LY 2484595;LY-2484595;trans-4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl)(2-methyl-2h-tetrazol-5-yl)amino)-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl)methyl)cyclohexanecarboxylic acid |
