DAGLβ-IN-1 is a universal intermediate for designing DAGL tailored activity-based probes, and is an inhibitor of diacylglycerol lipase-β (DAGLβ).

In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. O-7460 is a selective inhibitor of 2-AG biosynthesis via DAGLα (IC50 = 690 nM). It demonstrates much weaker inhibition towards human monoacylglycerol lipase and rat brain fatty acid amide hydrolase (IC50s > 10 μM) and does not bind to CB1 or CB2 cannabinoid receptors (Kis > 10 μM). At 0-12 mg/kg, i.p. in mice, O-7460 was reported to dose-dependently inhibit high-fat diet intake and reduce body weight.

Orlistat (Tetrahydrolipstatin) is an Intestinal Lipase Inhibitor. The mechanism of action of orlistat is as a Lipase Inhibitor.