96829-58-2

Orlistat (Tetrahydrolipstatin) is a lipase inhibitor and a fatty acid synthase (FASN) inhibitor. Orlistat has been shown to promote weight loss.

Orlistat-D3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat (T0686) is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-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 (T0686) 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; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (T0686) (10 mg/kg) decreases serum cholesterol levels and total bod......

(R,S,S,S)-Orlistat is a stereoisomeric derivative of orlistat (Tetrahydrolipstatin; THL) that inhibits three mycobacterial lipid esterases: Ag85C (KI: 16.43 μM), Rv3802 (EC50: 16.2 nM), and Pks13-TE.