Orlistat

Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase alpha (DAGLalpha), DAGLbeta, alpha/beta-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH, IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM. It also inhibits fatty acid synthase (FASN, apparent Ki = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (10 mg/kg) decreases serum cholesterol levels and total body weight in a mouse model of obesity induced by a high-fat diet. Formulations containing orlistat have been used in the treatment of adult obesity.Formal Name: N-formyl-L-leucine-(1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester. CAS Number: 96829-58-2. Synonyms: Ro 18-0647/002, (-)-Tetrahydrolipstatin. Molecular Formula: C29H53NO5. Formula Weight: 495.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 10 mg/ml, Ethanol: 20 mg/ml. SMILES: CCCCCCCCCCC[C@H](OC([C@@H](NC([H])=O)CC(C)C)=O)C[C@@H]1OC([C@H]1CCCCCC)=O. InChi Code: InChI=1S/C29H53NO5/c1-5-7-9-11-12-13-14-15-16-18-24(34-29(33)26(30-22-31)20-23(3)4)21-27-25(28(32)35-27)19-17-10-8-6-2/h22-27H,5-21H2,1-4H3,(H,30,31)/t24-,25-,26-,27-/m0/s1. InChi Key: AHLBNYSZXLDEJQ-FWEHEUNISA-N.