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CAS NO.96829-58-2
99%(1-10)Kilogram
96829-58-2 in stock 96829-58-2 On Sale Orlistat Hot Sale
Orlistat is an internationally recognized new form of weight loss drug. Its commercial name is Sainike and first went on sale in New Zealand in 1998. Orlistat is a long-term and highly effective specific gastrointestinal lipase inhibitor, and it is insoluble in water, soluble in chloroform, and easily soluble in ethanol.
Orlistat can be used clinically to treat obesity. Usually, a dose of 120mg is taken three times a day within one hour of a meal. Weight loss begins to occur after two weeks of usage. It can be used continuously for 6-12 months, and its effects will cease to increase after daily dosage exceeds 400mg. This drug is suitable to be used in combination with a low-calorie diet by obese and overweight individuals, and it can also be used as long-term treatment for patients who have faced weight-related risk factors. Orlistat has a long-term weight-control effect that reduces and maintains weight and prevents against rebounding. Using Orlistat can lower the occurrences of weight-related risk factors and diseases, including hypercholesterolemia, type-2 diabetes, impaired glucose tolerance, hyperinsulinemia, and hypertension, and it can reduce the fat content in organs. Orlistat also adjusts blood lipid levels: it can decrease serum triglycerides (TG) and low density lipoprotein cholesterol (LDL-C), and it can increase the ratio of high density lipoproteins to low density lipoproteins in obese patients.
Orlistat is a hypolipemic pancreatic, gastric and carboxylester lipase inhibitor. Exhibits no activity at phospholipase A2, liver esterase, trypsin and chymotrypsin. Inhibits the thioesterase domain of fatty acid synthase, leading to cell cycle arrest at the G1/S boundary in vitro. Prevents the absorption of approximately one third of fat from food and exhibits progastrokinetic, antiobesity and antihypercholesterolemic activity in vivo.
Orlistat 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 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 (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.