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