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    Anacetrapib (MK-0859)
    Anacetrapib (MK-0859)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0911
    CAS #: 875446-37-0Purity ≥98%

    Description: Anacetrapib (formerly also known as MK0859) is a novel, potent, selective, reversible inhibitor of rhCETP (Cholesteryl ester transfer protein) and mutant CETP(C13S) with IC50 of 7.9 nM and 11.8 nM, it increases HDL-C and decreases LDL-C, and does not increase aldosterone or blood pressure. It is being developed for the treatment of hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. Cholesteryl ester transfer protein, also called plasma lipid transfer protein, is a plasma protein that facilitates the transport of cholesteryl esters and triglycerides between the lipoproteins.

    References: J Lipid Res. 2010 Dec;51(12):3443-54; J Lipid Res. 2010 Sep;51(9):2739-52.

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    Molecular Weight (MW)637.51
    FormulaC30H25F10NO3
    CAS No.875446-37-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 127 mg/mL (199.2 mM)
    Water: <1 mg/mL
    Ethanol: 127 mg/mL (199.2 mM)
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 10 mg/mL
    SynonymsMK 0859; Anacetrapib; MK0859; MK-0859; 


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    In Vitro

    In vitro activity: Anacetrapib is not only able to increase HDL-cholesterol, but also further decreases LDL-cholesterol when taken in combination with a statin. Anacetrapib dose-dependently and significantly decreases the transfer of CE from HDL3 to HDL2. Anacetrapib doesn't affect the amount of [14C]-dalcetrapibthiol bound to rhCETP. Anacetrapib decreases pre-β-HDL formation by more than 46%. Anacetrapib potently blocks CE and TG transfer in 95% human serum.


    Kinase Assay: The inhibitory potency (IC50) of Dalcetrapib, Torcetrapib, and Anacetrapib to decrease CE transfer from HDL to LDL by rhCETP and C13S CETP is measured using a scintillation proximity assay kit. Briefly, [3H]CE-labeled HDL donor particles are incubated in the presence of purified CETP proteins (final concentration 0.5 µg/mL) and biotinylated LDL acceptor particles for 3 h at 37°C. Subsequently, streptavidin-coupled polyvinyltoluene beads containing liquid scintillation cocktail binding selectively to biotinylated LDL are added, and the amount of [3H]CE molecules transferred to LDL is measured by β counting. 


    Cell Assay: Cells are seeded in a 96 well plate overnight prior to the treatment by different concentrations of CETP inhibitors (e.g., Anacetrapib) for 24 h. Cell viability is measured using the CellTiter-Glo Luminescent Cell Viability Assay kit. Four wells are evaluated under each experimental condition.

    In VivoIn a dyslipidemic hamster model, 60 mg/kg/day Anacetrapib for 2 weeks results in a 94% reduction in CETP activity and 47% increase in HDL-cholesterol compared with control animals; non-HDL-cholesterol concentrations are not affected. In addition, Anacetrapib promotes reverse cholesterol transport from macrophages, and leads to a 30% increase in fecal cholesterol content. HDL from Anacetrapib-treated hamsters reveals an increase in SR-B1- and ABCG1-mediated efflux compared with controls. After oral administration of [14C]Anacetrapib at 10 mg/kg, ∼80 and 90% of the radioactive dose is recovered over 48 hous postdose from rats and monkeys, respectively. The majority of the administered radioactive dose is excreted unchanged in feces in both species.
    Animal modelAdult male Sprague-Dawley rats
    Formulation & DosageDissolved in polyethylene glycol 300-water (7:3, v/v); 2.5 mL/kg (2.5, 25, 50, 250 mg/mL); oral gavage
    ReferencesJ Lipid Res. 2010 Dec;51(12):3443-54; J Lipid Res. 2010 Sep;51(9):2739-52.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Anacetrapib (MK-0859)

    [3H]cholesteryl ester-labeled HDL3 was incubated with unlabeled HDL2 and recombinant human cholesteryl ester transfer protein [(rh)CETP] in the presence of: (A) dalcetrapib, 0.01 µM to 10 µM (n = 3); (B) dalcetrapib, 1 µM and 10 µM, torcetrapib and anacetrapib. J Lipid Res.2010 Dec;51(12):3443-54. 

    Anacetrapib (MK-0859)

    A: Competition of [14C]torcetrapib (0.25 μM) and unlabeled CETP inhibitors for binding to rhCETP. B: Displacement of [14C]dalcetrapib in the presence of reducing agent tris(2-carboxyethyl)phosphine (TCEP) by CETP inhibitors after preincubation. J Lipid Res. 2010 Dec;51(12):3443-54. 

    Anacetrapib (MK-0859)

    Schematic depicting action of CETP and proposed effects of dalcetrapib and torcetrapib. J Lipid Res.2010 Dec;51(12):3443-54.  


     

    Anacetrapib (MK-0859)

     

    Anacetrapib (MK-0859)

    A: Human plasma with an endogenous CETP level of 1.25 μg/ml was incubated for 21 h with and without test compounds, dalcetrapib, torcetrapib, and anacetrapib (0.1, 1, 3, and 10 µM). J Lipid Res.2010 Dec;51(12):3443-54. 

     


    Anacetrapib (MK-0859)

    Comparison of the effect of dalcetrapib, torcetrapib, and anacetrapib on HDL-C·AUC and radioactivity of fecal total sterols as a percentage of injected radioactivity in the hamster macrophage reverse cholesterol transport (RCT) study. J Lipid Res. 2010 Dec;51(12):3443-54.


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