96829-58-2

Orlistat (Tetrahydrolipstatin) 是一种脂肪酶 (lipase) 抑制剂，也是一种脂肪酸合成酶 (FASN) 抑制剂。Orlistat 具有促减肥的作用。

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......