1252765-13-1
1252765-13-1 structure
- Name: JNJ-42226314
- Chemical Name: JNJ-42226314
- CAS Number: 1252765-13-1
- Molecular Formula: C26H24FN5O2S
- Molecular Weight: 489.56
- Catalog: Signaling Pathways Metabolic Enzyme/Protease MAGL
- Create Date: 2020-04-05 13:55:00
- Modify Date: 2024-01-15 18:56:51
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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].
| Name | JNJ-42226314 |
|---|
| 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]. |
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| Related Catalog | |
| 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. |
| References |
| Molecular Formula | C26H24FN5O2S |
|---|---|
| Molecular Weight | 489.56 |