Product Name: Orlistat
Synonyms: (S)-2-FORMYLAMINO-4-METHYL-PENTANOIC ACID (S)-1-[[(2S, 3S)-3-HEXYL-4-OXO-2-OXETANYL]METHYL]-DODECYL ESTER; RO-18-0647; (-)-TETRAHYDROLIPSTATIN; ORLISTAT; N-FORMYL-L-LEUCINE (1S)-1-[[(2S, 3S)-3-HEXYL-4-OXO-2-OXETANYL]METHYL]DODECYL ESTER; XENICAL; (-)-Tetrahydrolipstatin(EquivalentToOrlistat); Orlipastat
CAS: 96829-58-2
MF: C29H53NO5
MW: 495.73
Product Categories: Pharmaceutical Raw Materials; Miscellaneous Biochemicals; API; Antiobesity Agent; Chiral Reagents; Intermediates & Fine Chemicals; Pharmaceuticals; Amino Acids & Derivatives; Heterocycles; ACTOS; Other APIs
mp < 50 °C
storage temp. 2-8°C
solubility DMSO: 19 mg/mL
form solid
color white
Chemical Properties : Off-White Solid

Product Description :

Orlistat is internationally recognized as a novel lipid-lowering diet drugs on the market under the trade name Xenical, available in New Zealand for the first time in 1998, when sales reached $ 146 million, 2007 sales of $ 538 million currently occupy orlistat weight loss market 80% of the global market share, China, Hong Kong only a year of sales reached $ 80 million.

Orlistat is a potent and specific long-term gastrointestinal lipase inhibitor, at room temperature for white or off-white powder, insoluble in water, soluble in chloroform, soluble in ethanol, with stomach and intestinal lumen active serine site of gastric lipase and pancreatic lipase to form a covalent bond to inactivate the enzyme. Dietary fat can not be broken down into free fatty acids and monoacylglycerols, so the fat can not be absorbed and utilized, thereby reducing the body's caloric intake, weight control. Systemic absorption of the drug without the need to play efficacy. Under usual dose, fat absorption can be suppressed by 30%. Rarely absorbed after oral administration, in the intestine may be metabolic inactivation, metabolism in the gastrointestinal tract wall portion, elimination half-life of about 14 to 19 hours. About 97% of the product with the feces, 83% of the prototype discharge.

Can be applied to clinical obesity and hyperlipidemia. Under normal circumstances, the time can be taken orally 120mg, three times a day in meal or one hour after a meal to take. Weight after taking two weeks to begin to decline. Continuous take 6 to 12 months, such as the dose increases to more than 400mg per day, and its role is no longer enhanced.

Application :

This product is suitable for low-calorie diet combined with mild obesity and overweight, including long-term treatment of obesity-related risk factors in patients who have already appeared. This product has a long-term weight control (weight loss, weight maintenance and prevention of rebound) effect. Taking orlistat can reduce the risk factors associated with obesity and obesity-related incidence of other diseases, including hypercholesterolemia, type Ⅱ diabetes, impaired glucose tolerance, hyperinsulinemia, hypertension, and reduce organ fat content.



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