Home Metabolism CETP inhibitor - LDL modulator Anacetrapib (MK-0859) For research use only.

Anacetrapib (MK-0859)

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.

Anacetrapib (MK-0859) Chemical Structure

Anacetrapib (MK-0859) Chemical Structure

CAS No. 875446-37-0

Purity & Quality Control

Anacetrapib (MK-0859) Related Products

Signaling Pathway

CETP Signaling Pathways

CETP Signaling Pathway

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
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 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]
Animal Research Animal Models Adult male Sprague-Dawley rats weighing 280 to 330 g
Dosages 2.5 mL/kg (2.5, 25, 50, 250 mg/mL)
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01122667 Completed
Dyslipidemia
Merck Sharp & Dohme LLC
 June 2010 Phase 1
NCT01114490 Completed
Dyslipidemia
Merck Sharp & Dohme LLC
 May 2010 Phase 1
NCT00325455 Terminated
Hypercholesterolemia|Mixed Hyperlipemia
Merck Sharp & Dohme LLC
 June 2006 Phase 2

Chemical Information & Solubility

Molecular Weight 637.51 Formula

C30H25F10NO3
CAS No. 875446-37-0 SDF Download Anacetrapib (MK-0859) SDF
Smiles CC1C(OC(=O)N1CC2=C(C=CC(=C2)C(F)(F)F)C3=CC(=C(C=C3OC)F)C(C)C)C4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (156.86 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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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