S80149 |
Evacetrapib (LY2484595) |
源葉(MedMol) | ≥98% |
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- 產品描述: Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
- 靶點: IC50: 5.5 nM (CETP)[1];CETP
- 體內研究:
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
- 參考文獻:
1. Cao G, 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.
- 溶解性: Soluble in DMSO
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.566 ml 7.829 ml 15.658 ml 5 mM 0.313 ml 1.566 ml 3.132 ml 10 mM 0.157 ml 0.783 ml 1.566 ml 50 mM 0.031 ml 0.157 ml 0.313 ml
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本計算器可幫助您計算出特定溶液中溶質的質量、溶液濃度和體積之間的關系,公式為:
質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)