Anacetrapib (MK-0859)

Catalog No.S2748

Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3.

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Anacetrapib (MK-0859) Chemical Structure

Anacetrapib (MK-0859) Chemical Structure
Molecular Weight: 637.51

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Anacetrapib (MK-0859) is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3.
Targets rhCETP [1] Mutant CETP (C13S) [1]
IC50 7.9 nM 11.8 nM
In vitro 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%. [1] Anacetrapib potently blocks CE and TG transfer in 95% human serum.[2]
In vivo In 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. [2] 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. [3]
Features

Protocol(Only for Reference)

Kinase Assay: [2]

Radioactive assays The ability of Anacetrapib to block CETP-mediated CE and TG transfer is measured by radioactive CETP transfer assay with 2% human serum. The procedure is similar to the 95% human serum transfer assay, except that purified human HDL (128 μg/mL) and [3H] cholesteryl oleate or [3H] triolein-labeled LDL are used as acceptor and donor particles, respectively. The [3H] cholesteryl oleate or [3H] triolein from exogenous LDL to HDL is transferred by purified recombinant CETP (30 nM) in standard CETP Buffer (50 mM Tris pH 7.4, 100 nM NaCl, and 1 mM EDTA) with 2% human serum. The transfer reaction is terminated by precipitation of LDL with one volume of ice cold human serum and 2 volumes of 20% W/V PEG 8000. The samples are centrifuged and an aliquot of the HDL-containing supernatant is counted by liquid scintillation. Counts present in the supernatant for controls (without CETP addition) are subtracted from those reactivated with CETP to correct for non-specific transfer.

Animal Study: [3]

Animal Models Adult male Sprague-Dawley rats weighing 280 to 330 g
Formulation In polyethylene glycol 300-water (7:3, v/v)
Dosages 2.5 mL/kg (2.5, 25, 50, 250 mg/mL)
Administration Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Niesor EJ, et al. J Lipid Res. 2010, 51(12), 3443-3454.

[2] Ranalletta M, et al. J Lipid Res. 2010, 51(9), 2739-2752.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01841684 Terminated Hyperlipoproteinemia Type II|Homozygous Familial Hypercholesterolemia Merck Sharp & Dohme Corp. June 2013 Phase 3
NCT01824238 Completed Heterozygous Familial Hypercholesterolemia (HeFH) Merck Sharp & Dohme Corp. May 2013 Phase 3
NCT01860729 Completed Hypercholesterolemia Merck Sharp & Dohme Corp. May 2013 Phase 3
NCT01760460 Completed Dyslipidemia Merck Sharp & Dohme Corp. March 2013 Phase 3
NCT01717300 Completed Hypercholesterolemia Merck Sharp & Dohme Corp. November 2012 Phase 3

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Chemical Information

Download Anacetrapib (MK-0859) SDF
Molecular Weight (MW) 637.51
Formula

C30H25F10NO3

CAS No. 875446-37-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 127 mg/mL (199.21 mM)
Ethanol 127 mg/mL (199.21 mM)
Water <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 10 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-Oxazolidinone, 5-[3,5-bis(trifluoromethyl)phenyl]-3-[[4'-fluoro-2'-methoxy-5'-(1-methylethyl)-4-(trifluoromethyl)[1,1'-biphenyl]-2-yl]methyl]-4-methyl-, (4S,5R)-

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