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Evacetrapib (LY2484595)

In stock
Catalog No.
A4377
CETP inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$210.00
In stock
5mg
$147.00
In stock
10mg
$189.00
In stock
50mg
$679.00
In stock
200mg
$1,519.00
In stock

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Background

Evacetrapib is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) with IC50 value of 5.5nM [1].

As a benzazepine-based inhibitor of CETP, evacetrapib is developed to increase HDL cholesterol for the treatment of coronary artery disease. Evacetrapib is efficacious both in vitro and in vivo. The IC50 values of evacetrapib against CETP are 5.5nM and 26nM, respectively in the buffer assay using human recombinant CETP and in the plasma assay using human plasma CETP. In the animal model of human CETP/ApoAI double transgenic mouse line, oral administration of evacetrapib at 30mg/kg significantly inhibits the CETP activity as well as increases the level of HDL. Besides that, the ED50 value of evacetrapib is less than 5mg/kg. Compared to the previous inhibitors of CETP, evacetrapib has less side effects. It is found no to increase blood pressure Zucker diabetic fatty rats and not to induce aldosterone or cortisol synthesis in H295R cells [1].

References:
[1] Cao G, Beyer TP, Zhang Y, Schmidt RJ, Chen YQ, Cockerham SL, Zimmerman KM, Karathanasis SK, Cannady EA, Fields T, Mantlo NB. 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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt638.65
Cas No.1186486-62-3
FormulaC31H36F6N6O2
Solubility≥32.1 mg/mL in DMSO, ≥50.4 mg/mL in EtOH with ultrasonic, <2.05 mg/mL in H2O
Chemical Name4-[[(5S)-5-[[3,5-bis(trifluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-1-yl]methyl]cyclohexane-1-carboxylic acid
SDFDownload SDF
Canonical SMILESCC1=CC(=C2C(=C1)C(CCCN2CC3CCC(CC3)C(=O)O)N(CC4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F)C5=NN(N=N5)C)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Evacetrapib is a potent and selective inhibitor of cholesterylester transfer protein (CETP) with IC50 value of 5.5 nM.
Targets CETP          
IC50 5.5 nM          

Quality Control

Chemical structure

Evacetrapib (LY2484595)