Orlistat

Orlistat is a digestive lipase inhibitor.1,2,3 It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM.4 It also inhibits fatty acid synthase (FASN; apparent Ki = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner.5 Orlistat (10 mg/kg) decreases serum cholesterol levels and total body weight in a mouse model of obesity induced by a high-fat diet.6 Formulations containing orlistat have been used in the treatment of adult obesity.WARNING This product is not for human or veterinary use.

A digestive lipase inhibitor

495.7

≥98%

Biochemicals/Analytical Standards/Isotopically Labeled Standards/Deuterium/Small Molecule Inhibitors/Fatty Acid Metabolism/Glycerolipid Lipases

Formal_Name:N-formyl-L-leucine-(1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester;Synonyms:Ro 18-0647/002 (–)-Tetrahydrolipstatin

CCCCCCCCCCC[C@H](OC([C@@H](NC([H])=O)CC(C)C)=O)C[C@@H]1OC([C@H]1CCCCCC)=O

C29H53NO5

96829-58-2

≥ 4 years

DMF: 20 mg/ml DMSO: 10 mg/ml Ethanol: 20 mg/ml

1.Hadváry, P.,Lengsfeld, H., and Wolfer, H. Inhibition of pancreatic lipase in vitro by the covalent inhibitor tetrahydrolipstatin. Biochemistry Journal 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. American Journal of Physiology and Gastrointestinal Liver Physiology 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. Biochemica et Biophysica Acta 1761, 205-212 (2006).

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