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Orlistat

Chemical Structure : Orlistat

CAS No.: 96829-58-2

Orlistat ((–)-Tetrahydrolipstatin, Ro-18-0647)

Catalog No.: PC-20125Not For Human Use, Lab Use Only.

Orlistat ((–)-Tetrahydrolipstatin, Ro-18-0647) is a small molecule inhibitor of pancreatic and gastric lipase, inhibits DAGLα, DAGLβ, ABHD12, ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH) with IC50 of 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively.

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Biological Activity

Orlistat ((–)-Tetrahydrolipstatin, Ro-18-0647) is a small molecule inhibitor of pancreatic and gastric lipase, inhibits DAGLα, DAGLβ, ABHD12, ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH) with IC50 of 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively.
Orlistat does not inhibit fatty acid amide hydrolase (FAAH) with IC50 of >100 uM.
Orlistat (1 uM) decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells.
also inhibits fatty acid synthase (FASN; apparent Ki =0.1 µM)) and inhibits the proliferation of PC3 prostate cancer cells in a concentration-dependent manner.
Orlistat (10 mg/kg) decreases serum cholesterol levels and total body weight in a mouse model of obesity induced by a high-fat diet.

Physicochemical Properties

M.Wt 495.75
Formula C29H53NO5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-formyl-L-leucine-(1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester

References

1. Bisogno, T.et al. J. Cell Biol. 163(3), 463-468 (2003).

2. Hoover, H.S.et al. Bioorg. Med. Chem. Lett. 18(22), 5838-5841 (2008).

3. Bisogno, T.,et al. Biochim. Biophys. Acta 1761(2), 205-212 (2006).

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