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Evacetrapib

Chemical Structure : Evacetrapib

CAS No.: 1186486-62-3

Evacetrapib (LY2484595;LY 2484595;LY-2484595)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 638.65
Formula C31H36F6N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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-

References

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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