Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : JNJ-42226314
CAS No.: 1252765-13-1
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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $118 | In stock | |
| 10 mg | $168 | In stock | |
| 25 mg | $258 | In stock | |
| 50 mg | $398 | In stock | |
| 100 mg | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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 | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
(1-(4-Fluorophenyl)-1H-indol-5-yl)(3-(4-(thiazole-2-carbonyl)piperazin-1-yl)azetidin-1-yl)methanone |
|
1. Ryan M Wyatt, et al. J Pharmacol Exp Ther. 2020 Mar;372(3):339-353.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
