Dalcetrapib

211513-37-0

C23H35NO2S

DMSO : >= 50 mg/mL (128.34 mM); H2O : < 0.1 mg/mL (insoluble)

Metabolic Enzyme/Protease

Dalcetrapib (JTT-705; RO-4607381) is a rhCETP inhibitor with IC50 of 0.2 uM that increases the plasma HDL cholesterol. IC50 value: 0.2 uM [1] Target: CETP in vitro: Dalcetrapib modulates CETP activity. Dalcetrapib induces a conformational change in CETP, when added to human plasma. CETP-induced pre-beta-HDL formation in human plasma is unchanged by Dalcetrapib <=3 uM and increased at 10 uM. Dalcetrapib statistically and significantly increases pre-beta-HDL formation [1]. Dalcetrapib achieves 50% inhibition of CETP activity in human plasma at a concentration of 9 uM [2]. Dalcetrapib inhibits the CETP activity of media in HepG2 in a dose-dependent manner [3]. in vivo: Treatment with Dalcetrapib leads to significant increases in HDL-C levels. In hamsters injected with [3H]cholesterol-labeled autologous macrophages Dalcetrapib significantly increases fecal elimination of both [3H]neutral sterols and [3H]bile acids. Dalcetrapib increases plasma HDL-[3H]cholesterol [1]. Dalcetrapib has 95% inhibition of CETP activity in male Japanese white rabbits at an oral dose of 30 mg/kg. Dalcetrapib increases the plasma HDL cholesterol level by 27% and 54%, respectively, when given at oral doses of 30 mg/kg or 100 mg/kg once a day for 3 days to male Japanese white rabbits [2].