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Orlistat

Cayman Chemical Item Number 10005426

Xenical™; Tetrahydrolipstatin; Alli (CAS 96829-58-2)

Orlistat (CAS 96829-58-2)

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Description

Orlistat inhibits gastric, pancreatic, and carboxyl ester lipases, preventing the hydrolysis of triglycerides to free fatty acids and monoglycerides, and as such is widely used to treat obesity.1 With a 120 mg dose before each meal in healthy subjects, orlistat is reported to accelerate gastric emptying and attenuates the secretion of glucose-dependent insulinotropic peptide without affecting plasma responses of cholecystokinin, glucagon-like peptide-1, pancreatic polypeptide, or insulin. 2 It also targets additional serine hydrolases in the nervous system, such as diacylglycerol lipase (DAGL), which is responsible for the conversion of DAG to 2-AG. Orlistat potently inhibits human recombinant DAGLα with an IC50 value of 60 nM and at 1 µM inhibits the formation of 2-AG in intact cells in vitro.3

1 Hadváry, P., Lengsfeld, H., and Wolfer, H. Inhibition of pancreatic lipase in vitro by the covalent inhibitor tetrahydrolipstatin. Biochem J 256 357-361 (1988).

2 Enç, F.Y., Önes, T., Akin, H.L., et al. Orlistat accelerates gastric emptying and attenuates GIP release in healthy subjects. Am J Physiol Gastrointest Liver Physiol 296 G482-G489 (2009).

3 Bisogno, T., Cascio, M.G., Saha, B., et al. Development of the first potent and specific inhibitors of endocannabinoid biosynthesis. Biochem Biophys Acta 1761 205-212 (2006).

Synonyms
  • Xenical™
  • Tetrahydrolipstatin
  • Alli
Formal Name N-​formyl-​L-​leucine-​(1S)-​1-​[[(2S,​3S)-​3-​hexyl-​4-​oxo-​2-​oxetanyl]methyl]dodecyl ester
CAS Number 96829-58-2
Molecular Formula C29H53NO5
Formula Weight 495.7
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CCCCCCCCCCC[C@H]​(OC(C(NC([H]​)​=O)​CC(C)​C)​=O)​C[C@@H]​1OC([C@H]​1CCCCCC)​=O

Background Reading

Hadváry, P., Lengsfeld, H., and Wolfer, H. Inhibition of pancreatic lipase in vitro by the covalent inhibitor tetrahydrolipstatin. Biochem J 256 357-361 (1988).

Bisogno, T., Cascio, M.G., Saha, B., et al. Development of the first potent and specific inhibitors of endocannabinoid biosynthesis. Biochem Biophys Acta 1761 205-212 (2006).

Enç, F.Y., Önes, T., Akin, H.L., et al. Orlistat accelerates gastric emptying and attenuates GIP release in healthy subjects. Am J Physiol Gastrointest Liver Physiol 296 G482-G489 (2009).
Size Price Quantity Subtotal
50 mg $24.00 $0.00
100 mg $46.00 $0.00
250 mg $108.00 $0.00
500 mg $192.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-05-25. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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