| Name | Anacetrapib |
| 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. |
| Cell Research | 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]. |
| 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[1]. |
| In vitro | Anacetrapib, in combination with inhibin, increased both HDL-cholesterol levels and decreased LDL-cholesterol levels.Anacetrapib dose-dependently inhibited the conversion of CE from HDL3 to HDL2.Anacetrapib had no effect on the number of [14C]-dalcetrapibthiol bindings to human recombinant CETP.Ki8751 also inhibited PDGFRα, c-Kit and FGFR-2, with higher IC50 values of 40 nM-170 nM. Effect. |
| In vivo | Anacetrapib, in combination with inhibin, increased both HDL-cholesterol levels and decreased LDL-cholesterol levels.Anacetrapib dose-dependently inhibited the conversion of CE from HDL3 to HDL2.Anacetrapib had no effect on the number of [14C]-dalcetrapibthiol bindings to human recombinant CETP.Ki8751 also inhibited PDGFRα, c-Kit and FGFR-2, with higher IC50 values of 40 nM-170 nM. Effect. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (78.43 mM)
Ethanol : 57 mg/mL (89.4 mM)
|
| Keywords | Cholesteryl ester transfer protein | inhibit | Inhibitor | CETP | MK0859 | Anacetrapib | MK 0859 |
| Inhibitors Related | Granotapide | BMS-212122 | KD-026 | NAMI-A | Lomitapide | Dirlotapide | Obicetrapib | Dalcetrapib |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | Inhibitor Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Human Metabolite Library |
United States
