FR186054

FR186054 is an oral active acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with the IC50 of 99 nM. FR186054 shows hypocholesterolemic effect and can be used for study of hypercholesterolemia and atherosclerosis[1][2].

Product Specifications

CAS Number

[179053-90-8]

UNSPSC

12352005

Target

Acyltransferase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/fr186054.html

Smiles

O=C(N(CC1=CC=CC(C2=NNC=C2)=C1)CC3=CC=CC=C3)NC4=C(SC)N=C(C)C=C4SC

Molecular Formula

C26H27N5OS2

Molecular Weight

489.66

References & Citations

[1]Tanaka A, et al. Synthesis, X-ray crystal structure, and biological activity of FR186054, a novel, potent, orally active inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) bearing a pyrazole ring. Bioorg Med Chem Lett. 1998;8 (1) :81-86.|[2]Tanaka A, et al. Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N- (heteroaryl-substituted benzyl) -N'-arylureas. J Med Chem. 1998;41 (13) :2390-2410.