Orlistat_CAS号96829-58-2说明书_AbMole中国

化学数据

分子量分子式CAS号储存条件

495.73C29H53NO596829-58-23年 -20°C 粉末状

溶解性（25°C）

DMSO 99 mg/mLWater <1 mg/mLEthanol 99 mg/mL

生物活性

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 bacteriumStreptomyces toxytricini. However, due to simplicity and stability, orlistat rather than lipstatin was developed into an anti-obesity drug. In vitro experimentsdemonstrate 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.

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

小鼠

重量 (kg)体表面积 (m2)Km 系数

0.020.0073

动物 B的Km系数动物 A的Km系数

大鼠0.150.0256

兔1.80.1512

豚鼠0.40.058

仓鼠0.080.025

狗100.520

动物 A (mg/kg) = 动物 B (mg/kg) × 

例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。