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ChemicalBook--->CAS DataBase List--->1252765-13-1

1252765-13-1

1252765-13-1 Structure

1252765-13-1 Structure
IdentificationBack Directory
[Name]

JNJ-42226314
[CAS]

1252765-13-1
[Synonyms]

JNJ-42226314
JNJ42226314,JNJ 42226314
1-(4-Fluorophenyl)-5-indolyl][3-[4-(thiazole-2-carbonyl)-1-piperazinyl]-1-azetidinyl]methanone
Methanone, [4-[1-[[1-(4-fluorophenyl)-1H-indol-5-yl]carbonyl]-3-azetidinyl]-1-piperazinyl]-2-thiazolyl-
[Molecular Formula]

C26H24FN5O2S
[MDL Number]

MFCD32671350
[MOL File]

1252765-13-1.mol
[Molecular Weight]

489.56
Chemical PropertiesBack Directory
[Boiling point ]

624.9±65.0 °C(Predicted)
[density ]

1.44±0.1 g/cm3(Predicted)
[storage temp. ]

2-8°C
[solubility ]

DMSO: 2mg/mL, clear
[form ]

Solid
[pka]

5.68±0.70(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

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].
[Biological Activity]

Brain penetranthighly selective and potent reversible inhibitor of monoacylglycerol lipase (MAGL).


JNJ-42226314 is a brain penetranthighly selective and potent reversible inhibitor of monoacylglycerol lipase (MAGL)(IC50 = 1.1) th at exhibits antinociceptive efficacy in the r at models neuropathic and inflammatory pain. JNJ-42226314 elevates hippocampal 2-arachidonoylglycerol (2-AG) levels and prolongs wakefulness in rats.
[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]

[1] Wyatt RM, et al.Pharmacologic characterization of JNJ-42226314, [1-(4-fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a reversible, selective and potent monoacylglycerol lipase inhibitor.J Pharmacol Exp Ther. 2019 Dec 9. DOI:10.1124/jpet.119.262139
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