JNJ-42226314

• CAT Number: I016894
• CAS Number: 1252765-13-1
• Molecular Formula: C26H24FN5O2S
• Molecular Weight: 489.56
• Purity: ≥95%
• Synonyms: [1-(4-fluorophenyl)indol-5-yl]-[3-[4-(1,3-thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone
• InChI: InChI=1S/C26H24FN5O2S/c27-20-2-4-21(5-3-20)32-9-7-18-15-19(1-6-23(18)32)25(33)31-16-22(17-31)29-10-12-30(13-11-29)26(34)24-28-8-14-35-24/h1-9,14-15,22H,10-13,16-17H2
• InChIKey: IVOACCSOISMVBL-UHFFFAOYSA-N
• SMILES: C1CN(CCN1C2CN(C2)C(=O)C3=CC4=C(C=C3)N(C=C4)C5=CC=C(C=C5)F)C(=O)C6=NC=CS6

JNJ-42226314(CAT: I016894) is a competitive, highly selective, and reversible non-covalent inhibitor of monoacylglycerol lipase (MAGL), a key enzyme in endocannabinoid metabolism. It exhibits potent activity with IC₅₀ values of 1.13 nM (human HeLa), 1.88 nM (human PBMC), 0.67 nM (mouse brain), and 0.97 nM (rat brain). JNJ-42226314 dose-dependently enhances levels of the endocannabinoid 2-arachidonoylglycerol (2-AG), increases hippocampal 2-AG in vivo, and shows efficacy in neuropathic and inflammatory pain models. In rats, it demonstrates antinociceptive effects in the CFA model and significantly increases total wake time. MAGL half-life values are 11.4, 27.6, and 27.2 min in human, mouse, and rat, respectively.