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Chemical Structure : JNJ-42226314
Catalog No.: PC-72112Not For Human Use, Lab Use Only.
JNJ-42226314 (JNJ42226314) is a potent, highly selective and reversible MAGL inhibitor with IC50 of 1.13 nM (hMAGL).
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JNJ-42226314 (JNJ42226314) is a potent, highly selective and reversible MAGL inhibitor with IC50 of 1.13 nM (hMAGL).
JNJ-42226314 displays high selectivity against the serine hydrolase superfamily, as well as a panel of 50 binding assays for ion channels and receptors, including CB1 and CB2. JNJ-42226314 also shows MAGL across species (mouse, rat MAGL IC50=1 nM).
JNJ-42226314 inhibits MAGL in a competitive mode with respect to the 2-AG substrate.
JNJ-42226314 time- and dose-dependently bound to MAGL, indirectly led to CB1 occupancy by raising 2-AG levels, and raised norepinephrine levels in cortex in rodent brain.
JNJ-42226314 exhibited antinociceptive efficacy in both the rat complete Freund's adjuvant-induced radiant heat hypersensitivity and chronic constriction injury-induced cold hypersensitivity models of inflammatory and neuropathic pain, respectively.
JNJ-42226314 induced hippocampal synaptic depression, altered sleep onset, and decreased electroencephalogram gamma power at 30 mg/kg, significantly increased 2-AG and norepinephrine levels, and produced neuropathic antinociception without synaptic depression at 3 mg/kg.
| M.Wt | 489.569 | |
| Formula | C26H24FN5O2S | |
| Appearance | Solid | |
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1. Ryan M Wyatt, et al. J Pharmacol Exp Ther. 2020 Mar;372(3):339-353.
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