Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN). Orlistat is a compound 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. 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.
|Solubility (25°C)||DMSO 89 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Zaidatul Akmal Othman, et al. Antioxidants (Basel). Anti-Atherogenic Effects of Orlistat on Obesity-Induced Vascular Oxidative Stress Rat Model
 Giorgia Cioccoloni, et al. Int J Oncol. Influence of fatty acid synthase inhibitor orlistat on the DNA repair enzyme O6-methylguanine-DNA methyltransferase in human normal or malignant cells in vitro
 Steven J Kridel, et al. Cancer Res. Orlistat is a novel inhibitor of fatty acid synthase with antitumor activity
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