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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Metabolism>CETP inhibitors>Anacetrapib
Anacetrapib
  • Anacetrapib

Anacetrapib NEW

Price $34 $34 $48 $48 $80 $80
Package 1mg 1mg 2mg 2mg 5mg 5mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Anacetrapib CAS No.: 875446-37-0
Purity: 99.62% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameAnacetrapib
DescriptionAnacetrapib (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 ResearchAnacetrapib (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 AssayThe 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 vitroAnacetrapib, 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 vivoAnacetrapib, 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.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationH2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (78.43 mM)
Ethanol : 57 mg/mL (89.4 mM)
KeywordsCholesteryl ester transfer protein | inhibit | Inhibitor | CETP | MK0859 | Anacetrapib | MK 0859
Inhibitors RelatedGranotapide | BMS-212122 | KD-026 | NAMI-A | Lomitapide | Dirlotapide | Obicetrapib | Dalcetrapib
Related Compound LibrariesBioactive Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | Inhibitor Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Human Metabolite Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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