MAGL-IN-4 是选择性的、口服有效的、可透过血脑屏障的、可逆的单酰基甘油脂肪酶抑制剂，IC50=6.2 nM。它主要通过大脑中选择性抑制 MAGL 增加 2-花生四烯酰甘油水平来增强内源性大麻素信号。

MAGL-IN-4 is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.

MAGL-IN-4 showed potent in vitro MAGL inhibitory activity (IC50 6.2 nM), good oral absorption and blood-brain barrier penetration[1].

MAGL-IN-4 showed significant pharmacodynamic changes (2-arachidonoylglycerol increase and arachidonic acid decrease) at 0.3-10 mg/kg, po. in mice[1].

2135785-20-3

His121 ARG57

DMSO:88 mg/mL (241.21 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years