Anacetrapib (MK-0859)

Catalog No.S2748

Anacetrapib (MK-0859) Chemical Structure

Molecular Weight(MW): 637.51

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.

Size Price Stock Quantity  
In DMSO USD 690 In stock
USD 270 In stock
USD 370 In stock

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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]
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]

Protocol

Animal Research
+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 127 mg/mL (199.21 mM)
Ethanol 127 mg/mL (199.21 mM)
Water <1 mg/mL
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 Information

Molecular Weight 637.51
Formula

C30H25F10NO3

CAS No. 875446-37-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

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
NCT01860729 Completed Hypercholesterolemia Merck Sharp & Dohme Corp. May 2013 Phase 3
NCT01824238 Completed Heterozygous Familial Hypercholesterolemia (HeFH) 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
NCT01524289 Active, not recruiting Hyperlipoproteinemia Type II|Heterozygous Familial Hypercholesterolemia Merck Sharp & Dohme Corp. February 2012 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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CETP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID