Name: Evacetrapib (LY2484595)
Price: 368.00 USD

- Overview
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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].
    
    [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.
- Properties
  - Alternative Name
    
    4-[[(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
    
    CAS Number
    
    1186486-62-3
    
    Molecular Formula
    
    C31H36F6N6O2
    
    Molecular Weight
    
    638.65
    
    Appearance
    
    A solid
    
    Purity
    
    98.83%
    
    Solubility
    
    ≥32.1 mg/mL in DMSO; insoluble in H2O; ≥50.4 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Evacetrapib (LY2484595)

Evacetrapib (LY2484595)

Background

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