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Evacetrapib

CAS No. : 1186486-62-3

MCE 国际站：Evacetrapib

产品活性：Evacetrapib 是一种有效的选择性的 CETP 抑制剂，在人血浆中，抑制人重组 CETP 蛋白 (IC₅₀ 为 5.5 nM) 和 CETP 活性，IC₅₀ 为 36 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：CETP

In Vitro: Evacetrapib is a novel benzazepine-based CETP inhibitor. In the buffer CETP assay, the absolute potency of the compound is 5.5 nM. In the human plasma CETP assay, the CETP concentration is about 2 μg/mL (25 nM) and the 36 nM IC₅₀ value again indicates that Evacetrapib is a potent CETP inhibitor against either the recombinant protein or CETP from human plasma. Evacetrapib is apparently much more potent than Dalcetrapib.

In Vivo: In double transgenic mice expressing human CETP and apoAI, Evacetrapib exhibits an ex vivo CETP inhibition ED₅₀ of less than 5 mg/kg at 8 h post oral dose and significantly elevated HDL cholesterol. Importantly, no blood pressure elevation is observed in rats dosed with Evacetrapib at high exposure multiples compared with the positive control, torcetrapib. Evacetrapib administered orally at 30 mg/kg results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4, 8 and 24 h post dose respectively. Evacetrapib dosed orally at 30 mg/kg resulted in 129.7% increase in HDL-C 8 h after oral administration.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Anti-diabetic Compound Library  |  Anti-Cardiovascular Disease Compound Library  |  Lipid Metabolism Compound Library   |  Targeted Diversity Library  |  Highly Selective Inhibitors Library  |  Torcetrapib  |  TAP311  |  CETP-IN-4  |  Dalcetrapib  |  Anacetrapib  |  MK-8262  |  CKD-519  |  CETP-IN-3  |  CP-532623  |  BMS-795311

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货号: HY-13327

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