Brief Description

LY2484595 is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure.
IC50 value: 5.5 nM
Target: CETP
LY2484595 inhibits human plasma CETP protein with IC50 of 26 nM. LY2484595 (< 10 μM) does not induce aldosterone or cortisol synthesis in H295R cells.
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. 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 LY2484595 in two dose-response studies are calculated to be 3.5 mg/kg and 4.1 mg/kg respectively. LY2484595 (< 200 mg/kg) does not increase blood pressure in Zucker diabetic fatty rats.

Solubility

DMSO 12.5 mg/ml

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

Light yellow to yellow solid