Description
Dalcetrapib is an inhibitor of rhCETP with IC50 value of 0.2 μM.
Product Overview
IC50: 6 μM for CETP inhibition in human plasma. Cholesteryl ester transfer protein (CETP) is a plasma protein that transfers neutral lipids among the lipoproteins. Its most important action is the exchange of cholesteryl esters in high-density lipoprotein (HDL)for triglycerides in very low-density lipoprotein. Thus, CETP is a potentially atherogenic protein, and its atherogenicity has been supported by many studies. Dalcetrapib is a novel inhibitors of CETP. Clinical trials: In a phase II study, Dalcetrapib showed no evidence of a pathological effect related to the arterial wall over 24 months. Moreover, this trial suggests possible beneficial vascular effects of dalcetrapib, including the reduction in total vessel enlargement over 24 months, but long-term safety and clinical outcomes efficacy of dalcetrapib need to be analysed.
Molecular Formula
C23H35NO2S
Chemical Name
S-[2-[[1-(2-ethylbutyl)cyclohexanecarbonyl]amino]phenyl] 2-methylpropanethioate
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
In vitro
Dalcetrapib achieved 50% inhibition of CETP activity in human plasma at a concentration of 6 μM. The mechanism of action was considered to involve the formation of a disulfide bond between the thiol form of Dalcetrapib and the cysteine residue at position 13 (Cys13) of CETP.
In vivo
Dalcetrapib achieved 95% inhibition of CETP activity in male Japanese white rabbits at an oral dose of 30 mg/kg. It increased the plasma HDL cholesterol level by 27% and 54%, respectively, when given at oral doses of 30 or 100 mg/kg once a day for 3 days to male Japanese white rabbits.
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