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Cat. No. M3549
Orlistat Structure

Tetrahydrolipstatin; Ro-18-0647

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
50mg USD 40  USD40 In stock
100mg USD 60  USD60 In stock
200mg USD 90  USD90 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 495.73
Formula C29H53NO5
CAS Number 96829-58-2
Solubility (25°C) DMSO 89 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.


[1] Zaidatul Akmal Othman, et al. Antioxidants (Basel). Anti-Atherogenic Effects of Orlistat on Obesity-Induced Vascular Oxidative Stress Rat Model

[2] 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

[3] Steven J Kridel, et al. Cancer Res. Orlistat is a novel inhibitor of fatty acid synthase with antitumor activity

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Keywords: Orlistat, Tetrahydrolipstatin; Ro-18-0647 supplier, FAS, inhibitors, activators

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