Orlistat (96829-58-2) is a lipase inhibitor which blocks the biosynthesis of 2-AG by inhibition of DAG lipase-α1. Inhibits pancreatic lipase and other lipases but not PLA22. Inhibits fatty acid synthase and displays antitumor activity3. Orlistat prevents fat absorption in the gut and is a clinically useful antiobesity agent4.
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2) Hadvary et al. (1991), The lipase inhibitor tetrahydrolipstatin bind covalently to the putative active site serine of pancreatic lipase; J. Biol. Chem., 266 2021
3) Kridel et al. (2004), Orlistat is a novel inhibitor of fatty acid synthase with antitumor activity; Cancer Res., 64 2070
4) Ballinger & Peikin (2002), Orlistat: it’s current status as an anti-obesity drug; Eur. J. Pharmacol., 440 109