Anacetrapib

• Description :

  Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.

• Product Name Alternative :

  MK-0859

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  PCSK9

• Type :

  Reference compound

• Related Pathways :

  Metabolic Enzyme/Protease

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Cardiovascular Disease

• Assay Protocol :

  https://www.medchemexpress.com/Anacetrapib.html

• Purity :

  99.25

• Solubility :

  DMSO : ≥ 100 mg/mL

• Smiles :

  O=C1O[C@@H]([C@@H](N1CC2=CC(C(F)(F)F)=CC=C2C3=CC(C(C)C)=C(C=C3OC)F)C)C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4

• Molecular Formula :

  C30H25F10NO3

• Molecular Weight :

  637.51

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Niesor EJ, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010, 51 (12), 3443-3454.|[2]Dong B, et al. CETP inhibitors downregulate hepatic LDL receptor and PCSK9 expression in vitro and in vivo through a SREBP2 dependent mechanism. Atherosclerosis. 2014 Aug;235 (2) :449-62.|[3]Tan EY, et al. Pharmacokinetics, metabolism, and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in rats and rhesus monkeys. Drug Metab Dispos. 2010, 38 (3), 459-473.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 3

• CAS Number :

  [875446-37-0]