Evacetrapib

SKU: orb1300926

Description

Evacetrapib

Research Area

Metabolism Research

Key Properties

• CAS Number: 1186486-62-3
• MW: 638.65
• Purity: 98.53%
• Formula: C₃₁H₃₆F₆N₆O₂
• SMILES: Cc1cc(C)c2N(C[C@H]3CC[C@@H](CC3)C(O)=O)CCC[C@H](N(Cc3cc(cc(c3)C(F)(F)F)C(F)(F)F)c3nnn(C)n3)c2c1
• Target: CETP
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:13 mg/mL (20.36 mM);Ethanol:11 mg/mL (17.22 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.13 mM)

Bioactivity

• Target IC50:
  CETP:5.5 nM
• In Vivo:
  Evacetrapib (LY2484595) (30 mg/kg, orally) results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4 hours, 8 hours and 24 hours post dose respectively in human ApoAI and CETP double transgenic mice. Evacetrapib (LY2484595) (30 mg/kg) results in 129.7% increase in HDL-C 8 hours after oral administration. The ED50 values of CETP inhibitory activity 8 hours post oral dosing for Evacetrapib (LY2484595) in two dose-response studies are calculated to be 3.5 mg/kg and 4.1 mg/kg respectively. Evacetrapib (LY2484595) (< 200 mg/kg) does not increase blood pressure in Zucker diabetic fatty rats.
• In Vitro:
  Evacetrapib (LY2484595) inhibits human plasma CETP protein with IC50 of 26 nM. Evacetrapib (LY2484595) (< 10 μM) does not induce aldosterone or cortisol synthesis in H295R cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, LY 2484595, LY2484595, LY-2484595, Evacetrapib, Inhibitor, CETP, Cholesteryl ester transfer protein

Compound Identifiers

PubChem CID

49836058