Anacetrapib

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 Specifications

CAS Number

[875446-37-0]

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.