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首页-小分子抑制剂&激动剂-Others-CETP-Evacetrapib
Evacetrapib

Chemical Structure : Evacetrapib

CAS No.: 1186486-62-3

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Evacetrapib (LY2484595, LY-2484595)

货号: PC-43496Not For Human Use, Lab Use Only.

Evacetrapib (LY2484595) is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) with IC50of 5.5 nM for human recombinant CETP protein.

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10 mg ￥880 In stock
25 mg ￥1480 In stock
50 mg ￥2580 In stock
100 mg ￥4280 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Evacetrapib (LY2484595) is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) with IC50 of 5.5 nM for human recombinant CETP protein.
Evacetrapib (LY2484595) inhibits CETP activity in human plasma with IC50 of 36 nM.
Evacetrapib (LY2484595) shows no significant inhibition in the CEREP cell surface receptor screening, as well as the nuclear receptor panel.
Evacetrapib (LY2484595) exhibits an ex vivo CETP inhibition ED50 of < 5 mg/kg at 8 h post oral dose and significantly elevates HDL cholesterol in vivo.
Evacetrapib (LY2484595) is a potent and selective CETP inhibitor without torcetrapib-like off-target liabilities.

物理化学性质&存储条件

分子量 638.65
分子式 C31H36F6N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Cyclohexanecarboxylic acid, 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]-, trans-

参考文献

1. Cao G, et al. J Lipid Res. 2011 Dec;52(12):2169-76.

2. Nicholls SJ, et al. JAMA. 2011 Nov 16;306(19):2099-109.

3. Barter PJ, et al. J Lipid Res. 2012 Sep;53(9):1755-66.

4. Suico JG, et al. J Cardiovasc Pharmacol Ther. 2014 May;19(3):283-9.

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