PF-04620110

Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis. PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2. It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours. PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.Formal Name: trans-4-[4-(4-amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]-cyclohexaneacetic acid. CAS Number: 1109276-89-2. Molecular Formula: C21H24N4O4. Formula Weight: 396.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.2 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 220, 244, 293 nm. SMILES: OC(C[C@@H]1CC[C@@H](C2=CC=C(N3CCOC(N=CN=C4N)=C4C3=O)C=C2)CC1)=O. InChi Code: InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-. InChi Key: GEVVQZHMFVFGLN-HDJSIYSDSA-N.