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MAGL inhibitor compound 23 is an inhibitor of monoacylglycerol lipase (MAGL; IC50 = 80 nM).1 It is selective for MAGL over cannabinoid receptor 1 (CB1), CB2, fatty acid amide hydrolase (FAAH), α/β-hydrolase domain-containing protein 6 (ABHD6), and ABHD12 (IC50s = >10 μM). MAGL inhibitor compound 23 inhibits the growth of HCT116, MDA-MB-231, Caov-3, OVCAR-3, and SKOV3 cells (IC50s = 21, 7.9, 25, 57, and 15 μM, respectively) but not MRC5 cells (IC50 = >100 μM). It increases the levels of 2-arachidonoyl glycerol (2-AG; Item No. 62160) in mouse brain and plasma when administered at a dose of 50 mg/kg.
WARNING This product is not for human or veterinary use.
1. Optimization of a benzoylpiperidine class identifies a highly potent and selective reversible monoacylglycerol lipase (MAGL) inhibitor. J. Med. Chem. 62(4), 1932-1958 (2019).