Dalcetrapib

Research use only, not for human use.

Dalcetrapib, a rhCETP inhibitor (IC50=0.2 μM), increases the plasma HDL cholesterol.

Dalcetrapib, aslo known as JTT-705, is a CETP inhibitor. The drug was aimed at raising the blood levels of "good cholesterol" (cholesterol carried in HDL particles, aka HDL-C). Prevailing observations indicate that high HDL levels correlate with better overall cardiovascular health, though it remains unclear whether raising HDL levels consequently leads to an increase in cardiovascular health. Development of this drug was halted on May 7, 2012 “due to a lack of clinically meaningful efficacy.(In Vitro):Dalcetrapib (JTT-705) (0.1-10 μM; 21 h) dose-dependently increases pre-β-HDL formation.Dalcetrapib (0-30 μM; 24 h) inhibits the CETP activity of media in HepG2 in a dose-dependent manner.(In Vivo):Dalcetrapib (JTT-705) (30 or 100 mg/kg; p.o.; once a day for 3 days) increases plasma HDL cholesterol in rabbits.Dalcetrapib (100 mg/kg; i.g.; twice daily for 7 days) significantly increases fecal elimination of neutral sterols, bile acids, and plasma HDL-cholesterol.

Dalcetrapib (JTT-705) (0.1-10 μM; 21 h) dose-dependently increases pre-β-HDL formation.Dalcetrapib (0-30 μM; 24 h) inhibits the CETP activity of media in HepG2 in a dose-dependent manner.

Dalcetrapib (JTT-705) (30 or 100 mg/kg; p.o.; once a day for 3 days) increases plasma HDL cholesterol in rabbits.Dalcetrapib (100 mg/kg; i.g.; twice daily for 7 days) significantly increases fecal elimination of neutral sterols, bile acids, and plasma HDL-cholesterol. Animal Model:Male JW rabbits Dosage:30 or 100 mg/kg Administration:Oral administration, once a day for 3 days Result:Increased plasma HDL cholesterol by 27% and 54% at 30 mg/kg and 100 mg/kg, respectively.

JTT-705 | JTT705 | JTT 705 | RO-4607381

Angiogenesis

FGFR

rhCETP

Cardiovascular Disease|Metabolic Disease

——

211513-37-0

389.59

C23H35NO2S

>98% (HPLC)

DMSO : ≥ 50 mg/mL. 128.34 mM; H2O : < 0.1 mg/mL

c1(ccccc1NC(=O)C1(CC(CC)CC)CCCCC1)SC(=O)C(C)C

S-[2-[[1-(2-ethylbutyl)cyclohexanecarbonyl]amino]phenyl] 2-methylpropanethioate

(-20℃)

With Ice Pack

≥ 2 years