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Anacetrapib (MK-0859)
Cat No.
CEI-1213
Description
Anacetrapib is a potent, selective, reversible inhibitor of rhCETP and mutant CETP(C13S) with IC50 values of 7.9 nM and 11.8 nM, respectively.
Product Overview
Anacetrapib, also known as MK-0859, is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) that exhibits strong inhibition against CETP-mediated transfer of cholesteryl esters and triglycerides with values of inhibition constant IC50 of 16 nM and 29 nM respectively. Anacetrapib is mainly metabolized by CYP3A4 through O-demethylation, hydroxylation on the biphenyl moiety and hydroxylation on the isopropyl side chain resulting in three oxidative metabolites M1, M2 and M3 respectively. Anacetrapib is being investigated for the treatment of primary hypercholesterolemia and mixed hyperlipidemia due to its impressive effects to lower low-density lipoprotein (LDL) cholesterol levels and increase high-density lipoprotein (HDL) cholesterol levels without any associated major adverse events.
CAS No.
875446-37-0
Molecular Weight
637.51
Purity
0.9959
Storage
Store at -20°C
Synonyms
MK 0859, MK0859
Targets
rhCETP; mutant CETP(C13S)
IC50
7.9 nM; 11.8 nM
Molecular Formula
C30H25F10NO3
Chemical Name
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-(4-fluoro-2-methoxy-5-propan-2-ylphenyl)-5-(trifluoromethyl)phenyl]methyl]-4-methyl-1,3-oxazolidin-2-one
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
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