Anacetrapib

SKU: orb1307084

Description

Anacetrapib (MK-0859) is a potent and reversible inhibitor of CETP, with IC50 values of 7.9 nM for rhCETP and 11.8 nM for the C13S mutant. It blocks cholesteryl ester transfer from HDL to LDL/VLDL, elevating HDL-cholesterol and lowering LDL-cholesterol in serum. This mechanism has been investigated in both in vitro assays and in vivo preclinical models of dyslipidemia.

Research Area

Metabolism Research

Key Properties

• CAS Number: 875446-37-0
• MW: 637.51
• Purity: 99.87% (May vary between batches)
• Formula: C₃₀H₂₅F₁₀NO₃
• SMILES: COc1cc(F)c(cc1-c1ccc(cc1CN1[C@@H](C)[C@H](OC1=O)c1cc(cc(c1)C(F)(F)F)C(F)(F)F)C(F)(F)F)C(C)C
• Target: Others,CETP
• Solubility: DMSO:50 mg/mL (78.43 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+90% Corn Oil:2.5 mg/mL (3.92 mM);Ethanol:57 mg/mL (89.41 mM)

Bioactivity

• Target IC50:
  CETP (mutant, C13S):11.8 nM|CETP (recombinant human):7.9 nM
• 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.
• 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.
• Cell Research:
  Anacetrapib (ANA) is dissolved in DMSO and diluted with appropriate media. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CETP, Cholesteryl ester transfer protein, Anacetrapib, MK 0859, MK0859, MK-0859, Inhibitor, inhibit, Mutant CETP (C13S), rhCETP

Compound Identifiers

PubChem CID

11556427