A-922500

Diacylglycerol acyltransferases (DGATs) catalyze the final step in triglyceride synthesis. DGAT-1 deficient mice demonstrate a phenotype that is protective against the development of diet-induced obesity (DIO) or insulin resistance, implicating the actions of this enzyme in the development of such metabolic disorders. A-922500 is a potent orally active inhibitor of DGAT-1 activity, inhibiting both human and mouse forms of the enzymes with IC50 values of 7 and 24 nM, respectively. When administered at 3 mg/kg to DIO mice, A-922500 conferred significant weight loss within seven days without affecting food intake and significantly reduced plasma and liver triglycerides with chronic dosing. A-922500 does not inhibit DGAT-2, ACAT-1, or ACAT-2.Formal Name: 2R-[[4'-[[(phenylamino)carbonyl]amino][1R,1'-biphenyl]-4-yl-carbonyl]-cyclopentanecarboxylic acid. CAS Number: 959122-11-3. Synonyms: (1R,2R)-2-(4'-(3-phenylureido)biphenylcarbonyl)-cyclopentanecarboxylic acid. Molecular Formula: C26H24N2O4. Formula Weight: 428.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml, Ethanol: 0.2 mg/ml. SMILES: O=C(NC1=CC=C(C2=CC=C(C([C@@H]3CCC[C@H]3C(O)=O)=O)C=C2)C=C1)NC4=CC=CC=C4. InChi Code: InChI=1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1. InChi Key: BOZRFEQDOFSZBV-DHIUTWEWSA-N.