URB602

URB602 is a selective inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC₅₀ value of 28 µM for the rat brain enzyme.¹ It does not inhibit fatty acid amide hydrolase (FAAH) at concentrations up to 100 µM or other lipid metabolizing enzymes such as diacylglycerol lipase or COX-2.^1,2 Inhibition of MAGL inhibits 2-arachidonoyl glycerol (Item No. 62160) hydrolysis, which is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.¹ URB602 (50 µM) also inhibits glucose-stimulated and depolarization-induced insulin secretion in INS-1 cells.³

WARNING This product is not for human or veterinary use.

1. Hohmann, A.G., Suplita, R.L., Bolton, N.M., et al. An endocannabinoid mechanism for stress-induced analgesia. Nature 435(7045), 1108-1112 (2005).

2. Tarzia, G., Duranti, A., Tontini, A., et al. Design, Synthesis, and strcture-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors. J. Med. Chem. 46, 2352-2360 (2003).

3. Berdan, C.S., Erion, K.A., Burritt, N.E., et al. Inhibition of monoacylglycerol lipase activity decreases glucose-stimulated insulin secretion in INS-1 (832/13) cells and rat islets. PLoS One 11(2), e0149008 (2016).