SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation.
体内研究:
SAR629 is a potent dual inhibitory action on MAGL and fatty acid amide hydrolase (FAAH). SAR629 inhibits rodent monoglyceride lipase (MGL) activity at subnanomolar potencies (IC50 values of 1.1 nM and 219 pM in rat and mouse brain membranes, respectively).