Anacetrapib (codenamed MK-0859) is a potent cholesteryl ester transfer protein (CETP) inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. Anacetrapib binds reversibly and dalcetrapib covalently to CETP. Anacetrapib inhibited CETP-mediated cholesteryl ester and triglyceride transfer with similar potencies. Anacetrapib potently blocks CE and TG transfer in 95% human serum. Single doses of anacetrapib markedly and dose-dependently inhibited serum CETP activity with peak effects of approximately 90% inhibition at t(max) and approximately 58% inhibition at 24 h post-dose. In addition, Anacetrapib promotes reverse cholesterol transport from macrophages, and leads to a 30% increase in fecal cholesterol content.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL
Ethanol 100 mg/mL
Biochemical characterization of cholesteryl ester transfer protein inhibitors.
Ranalletta M, et al. J Lipid Res. 2010 Sep;51(9):2739-52. PMID: 20458119.
Single-dose pharmacokinetics and pharmacodynamics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.
Krishna R, et al. Br J Clin Pharmacol. 2009 Oct;68(4):535-45. PMID: 19843057.
|Related CETP Products|
Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol.
Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP which inhibited human recombinant CETP protein (5.5 nM IC(50)) and CETP activity in human plasma (36 nM IC(50)) in vitro.
Torcetrapib (CP-529414) is a prototype cholesteryl ester transfer protein (CETP) inhibitor with potential for decreasing atherosclerotic disease, increased cardiovascular events in clinical trials.
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