CAS NO: | 875446-37-0 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
Molecular Weight (MW) | 637.51 |
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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 | MK 0859; Anacetrapib; MK0859; MK-0859; |
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 doesn't 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: The inhibitory potency (IC50) of Dalcetrapib, Torcetrapib, and Anacetrapib to decrease CE transfer from HDL to LDL by rhCETP and C13S CETP is measured using a scintillation proximity assay kit. Briefly, [3H]CE-labeled HDL donor particles are incubated in the presence of purified CETP proteins (final concentration 0.5 μg/mL) and biotinylated LDL acceptor particles for 3 h at 37°C. Subsequently, streptavidin-coupled polyvinyltoluene beads containing liquid scintillation cocktail binding selectively to biotinylated LDL are added, and the amount of [3H]CE molecules transferred to LDL is measured by β counting. Cell Assay: Cells are seeded in a 96 well plate overnight prior to the treatment by different concentrations of CETP inhibitors (e.g., Anacetrapib) for 24 h. Cell viability is measured using the CellTiter-Glo Luminescent Cell Viability Assay kit. Four wells are evaluated under each experimental condition. |
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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. |