| Description | FR-186054 is a new, potent inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) and has oral activity. Compared to other ACAT inhibitors, this compound displayed excellent in vitro efficacy, irrespective of dosing method, indicating superior characteristics. |
| Synonyms | FR186054, FR 186054 |
| molecular weight | 489.66 |
| Molecular formula | C26H27N5OS2 |
| CAS | 179053-90-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Tanaka A, Terasawa T, Hagihara H, Kinoshita T, Sakuma Y, Ishibe N, Sawada M, Takasugi H, Tanaka H. 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 Jan 6;8(1):81-6. PubMed PMID: 9871633. 2. Tanaka A, Terasawa T, Hagihara H, Sakuma Y, Ishibe N, Sawada M, Takasugi H, Tanaka H. 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 Jun 18;41(13):2390-410. PubMed PMID: 9632372. |