| Description |
A membrane-permeable carbamate that acts as a highly potent and selective inhibitor against the 2-acetyl MAGE (monoakylglycerol ether) hydrolase KIAA1363/AADACL1 of both human (IC 50 = 12 nM; PC3 cell lysate) and murine (IC 50 = 20 nM; mouse brain membrane homogenate) origin, presumably via covalent/irreversible carbamoylation of enzyme active site nucleophilic serine, with no significant effect toward other PC3 or murine brain serine hydrolase activities, including HSL, FAAH, and AChE. Readily crosses blood-brain barrier in mice (complete inhibition of brain KIAA1363 in 4 h after single i.p. or o.g./oral gavage dose of 5 mg/kg and 20 mg/kg, respectively)
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