| Description | Anacetrapib (MK-0859) (MK0859) is an effective, specific, reversible rhCETP and mutant CETP(C13S) inhibitor (IC50: 7.9 nM and 11.8 nM). Anacetrapib reduces the transfer of cholesteryl ester from HDL to LDL and/or VLDL thereby, producing an increase in serum HDL-cholesterol levels and a decrease in serum LDL-cholesterol levels. |
| In vitro | Anacetrapib对巨噬细胞胆固醇逆向转运有促进作用,可增加30%的排泄物胆固醇含量.处理异常仓鼠模型,持续处理2周,与对照组相比,Anacetrapib （60 mg/kg/day）使CETP活性下降94%,HDL-胆固醇上升47%,不影响非HDL胆固醇浓度.与对照组相比,Anacetrapib处理的仓鼠HDL显示ABCG1和SR-B1调节的流出物增多. [14C]Anacetrapib（10 mg/kg,p.o.）给药48 h后,鼠和猴分别恢复～80和90%放射性,但排泄物中放射性几乎无变化. |
| In vivo | Anacetrapib和抑制素联用时,既可提高HDL-胆固醇水平,也可降低LDL-胆固醇水平。Anacetrapib剂量依赖性地抑制CE从HDL3转变为HDL2。Anacetrapib对[14C]-dalcetrapibthiol与人类重组CETP的结合数无影响。 |
| Cell experiments | Anacetrapib (ANA) is dissolved in DMSO and diluted with appropriate media[2]. 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[2]. |
| Target activity | CETP (mutant, C13S):11.8 nM, CETP (recombinant human):7.9 nM |
| Synonyms | 安塞曲匹, MK-0859 |
| molecular weight | 637.51 |
| Molecular formula | C30H25F10NO3 |
| CAS | 875446-37-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 50 mg/mL (78.43 mM) Ethanol: 57 mg/mL(89.4 mM) |
| References | 1. Niesor EJ, et al. J Lipid Res. 2010, 51(12), 3443-3454. 2. Ranalletta M, et al. J Lipid Res. 2010, 51(9), 2739-2752. 3. Tan EY, et al. Drug Metab Dispos. 2010, 38(3), 459-473. |