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JNJ-42226314

Chemical Structure : JNJ-42226314

CAS No.: 1252765-13-1

JNJ-42226314 (JNJ42226314)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 489.569
Formula C26H24FN5O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
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

References

1. Ryan M Wyatt, et al. J Pharmacol Exp Ther. 2020 Mar;372(3):339-353.

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