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Orlistat

Cat. No. M3549
Orlistat Structure
Synonym:

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
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 495.73
Formula C29H53NO5
CAS Number 96829-58-2
Purity 100.0%
Solubility DMSO 89 mg/mL
Storage at -20°C
References

[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

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