Anacetrapib (MK-0859)

Anacetrapib (MK-0859)

Catalog Number:
L002369173APE
Mfr. No.:
APE-A4375
Price:
$335
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      • Overview
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          Background

          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.

      • Properties
        • Alternative Name
          MK 0859, MK0859; (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
          CAS Number
          875446-37-0
          Molecular Formula
          C30H25F10NO3
          Molecular Weight
          637.51
          Appearance
          A solid
          Purity
          99.76%
          Solubility
          ≥31.9 mg/mL in DMSO; insoluble in H2O; ≥86.6 mg/mL in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Lee EY, Yoo JA, et al. "Anti-Aging and Tissue Regeneration Ability of Policosanol Along with Lipid-Lowering Effect in Hyperlipidemic Zebrafish via Enhancement of High-Density Lipoprotein Functionality." Rejuvenation Res. 2016 Apr;19(2):149-58. PMID:26413884

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