product name Anacetrapib (MK-0859)
Description: Anacetrapib (also known as MK0859) is a potent, selective, reversible inhibitor of rhCETP 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.
References: J Lipid Res. 2010 Dec;51(12):3443-54; J Lipid Res. 2010 Sep;51(9):2739-52.
637.51
Formula
C30H25F10NO3
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
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19406443
| 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 doesnt 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: Cell Assay: |
|---|---|
| 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. 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 model | Adult male Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in polyethylene glycol 300-water (7:3, v/v); 2.5 mL/kg (2.5, 25, 50, 250 mg/mL); oral gavage |
| References | J Lipid Res. 2010 Dec;51(12):3443-54; J Lipid Res. 2010 Sep;51(9):2739-52. |
