1. Metabolic Enzyme/Protease
  2. MAGL
  3. JNJ-42226314

JNJ-42226314 

Cat. No.: HY-133130
Handling Instructions

JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain.

For research use only. We do not sell to patients.

JNJ-42226314 Chemical Structure

JNJ-42226314 Chemical Structure

CAS No. : 1252765-13-1

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Description

JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain[1].

In Vitro

JNJ-42226314 has IC50s of 1.13 nM, 1.88 nM, 0.67 nM, 0.97 nM for human Hela cells, human PBMC, mouse brain and rat brain, respectively[1].

In Vivo

JNJ-42226314 (i.p.; 3 mg/kg and 30 mg/kg; 120 min) dose-dependently elevates hippocampal 2-AG in vivo[1].
JNJ-42226314 (i.p.; 30 mg/kg)significantly increases total wake time for up to 8 hours afterward, whereas total wake time was only elevated for 2 hr following a 3 mg/kg dose[1].
JNJ-42226314 (i.p.; 30 mg/kg) is antinociceptive in the rat complete Freund’s adjuvant (CFA) model of inflammatory pain[1].
JNJ-42226314 has t1/2 values of 11.4, 27.6, 27.2 min for MAGL in human, mouse and rat, respectively[1].

Animal Model: Male C57Bl/6 mice weighing 20-30g and male Sprague-Dawley rats weighing 300-400 g[1]
Dosage: 3 mg/kg and 30 mg/kg
Administration: i.p.; 120 min
Result: Dose-dependently elevated hippocampal 2-AG in vivo.
Molecular Weight

489.56

Formula

C₂₆H₂₄FN₅O₂S

CAS No.

1252765-13-1

SMILES

O=C(N1CCN(C2CN(C(C3=CC4=C(N(C5=CC=C(F)C=C5)C=C4)C=C3)=O)C2)CC1)C6=NC=CS6

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

JNJ-42226314JNJ42226314JNJ 42226314MAGLMonoacylglycerol lipasecompetitivereversiblenon-covalent2-arachidonoylglycerol2-AGneuropathicinflammatorypainInhibitorinhibitorinhibit

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JNJ-42226314
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HY-133130
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