Anacetrapib (MK-0859)

Catalog No.S2748

For research use only.

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

CAS No. 875446-37-0

Selleck's Anacetrapib (MK-0859) has been cited by 3 Publications

Purity & Quality Control

Choose Selective CETP Inhibitors

Other CETP Products

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 (from reference)

Animal Research: [3]
  • 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

Solubility (25°C)

In vitro

DMSO 127 mg/mL
(199.21 mM)
Ethanol 127 mg/mL
(199.21 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.

10 mg/mL

Chemical Information

Molecular Weight 637.51
Formula

C30H25F10NO3

CAS No. 875446-37-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01122667 Completed Drug: anacetrapib Dyslipidemia Merck Sharp & Dohme Corp. June 2010 Phase 1
NCT01114490 Completed Drug: anacetrapib Dyslipidemia Merck Sharp & Dohme Corp. May 2010 Phase 1
NCT00325455 Terminated Drug: MK0859 Hypercholesterolemia|Mixed Hyperlipemia Merck Sharp & Dohme Corp. June 2006 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Anacetrapib (MK-0859) | Anacetrapib (MK-0859) supplier | purchase Anacetrapib (MK-0859) | Anacetrapib (MK-0859) cost | Anacetrapib (MK-0859) manufacturer | order Anacetrapib (MK-0859) | Anacetrapib (MK-0859) distributor