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产品介绍
产品介绍
产品信息
抗原名称
lipase ,Fatty acid synthesis
商品描述
Orlistat is a drug that promotes loss of weight by preventing the digestion and absorption of fat in food. It is intended for use in conjunction with a physician-supervised reduced-calorie diet. Orlistat is the saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini. However, due to simplicity and stability, orlistat rather than lipstatin was developed into an anti-obesity drug. In vitro experiments demonstrate that orlistat has an IC50 of 122 ng/ml for PL from human duodenal juice, but an IC50 of about 300 ng/ml for LPL.
分子量
495.73
纯度
>98%
可溶性
Ethanol ：49.6 mg/mL (100 mM)
DMSO ：49.6 mg/mL (100 mM)
DMSO ：49.6 mg/mL (100 mM)
外观
白色或类白色粉末
In vitro(体外研究)
Orlistat, an inhibitor of lipases and fatty acid synthase, is used orally for long-term treatment of obesity. Orlistat shows antiproliferative activity against cancer cells in vitro. It has been found to augment pro-apoptotic NOXA protein.
In vivo(体内研究)
Orlistat, administered by oral route, is minimally absorbed by the gastrointestinal tract and is able to prevent the absorption of a large percentage of lipids, thereby reducing lipid supply from outside sources. Because of its extremely low oral bioavailability, the effects of Orlistat are largely confined to the gastrointestinal tract, where it inactivates pancreatic lipase. Therefore, the formulation and route of delivery would have to be changed to treat tumors of the breast, prostate, and so on. Orlistat halts tumor cell proliferation, induces tumor cell apoptosis, and inhibits the growth of PC-3 tumors in nude mice. A pharmacokinetic analysis of Orlistat (155 mg/kg) administered by i.p. injection showed peak blood levels to be ∼10 μM 2 h after dosing (data not shown). Beyond this time, blood levels of the drug decayed rapidly.
背景
别名
奥利司他；Tetrahydrolipstatin；Ro-18-0647
分子式
C29H53NO5
CAS号
96829-58-2
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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