产品描述:
ABX-1431 is an inhibitor of monoacylglycerol lipase (MAGL; IC50s = 14 and 27 nM for human and rat enzyme, respectively).{35416} It is selective for MAGL over ABHD6 and PLA2G7 (IC50s = 2.7 and >10 μM, respectively), as well as a panel of 33 serine hydrolases and a panel of 95 enzymes, receptors, transporters, and ion channels at 10 μM. It is also selective for MAGL over the cytochrome P450 (CYP) isoforms CYP1A2, CYP2C9, CYP2C19, and CYP3A4/5 (IC50s = >50 μM). Ex vivo, ABX-1431 inhibits MAGL activity in mouse and rat brain (ED50s = 1.4 and 0.5 mg/kg, respectively). In vivo, ABX-1431 decreases brain levels of 2-arachidonoyl glycerol (2-AG; Item No. 62160) in mice and rats and reduces formalin-induced paw-licking time in rats.