セチリスタット 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
効能
抗肥満薬, 膵リパーゼ阻害薬
商品名
オブリーン (武田薬品工業)
説明
Cetilistat (also known as ATL-962) was approved in September 2013 by the Japanese Ministry of Health, Labor and Welfare for the treatment of obesity, limited to patients with both type 2 diabetes mellitus (T2DM) and dyslipidemia, and with a body mass index (BMI)25 kg/m
2 in spite of dietary treatment and/or exercise therapy. As with orlistat, cetilistat works via inhibition of pancreatic lipases in the gut to inhibit fat absorption and thereby reduce caloric uptake from diet. The medicinal chemistry program has not been described in the scientific literature, but the patent describing cetilistat also describes the synthesis of analogs with varied aryl substituents and lipophilic tails. The synthesis of cetilistat involves condensation of a hexadecylcarbonochloridate with 2-amino-5-methylbenzoic acid; other analogs were synthesized by varying the carbonochloridate and 2-aminobenzoic acid components. Cetilistat is a potent inhibitor of human and rat pancreatic lipase with IC
50s of 15 and 136 nM, respectively, with little inhibition of trypsin or chymotrypsin.
化学的特性
Off-white Cryst
使用
A novel pancreatic lipase inhibitor for the treatment of obesity in both diabetic and non-diabetic patients.
作用機序
Orlistat and cetilistat are both gastrointestinal lipase inhibitors. They effectively inhibit the hydrolysis of dietary fat into fatty acids and monoglyceride in the gastrointestinal tract.52 Orlistat is reported to be able to reduce weight while improving lipid distribution, blood glucose, and blood pressure[1]. Specifically, it isdrugs blocking fat absorption.
セチリスタット 上流と下流の製品情報
原材料
準備製品