ChemicalBook CAS DataBase List 1252765-13-1

1252765-13-1

Name	JNJ-42226314
CAS	1252765-13-1
Molecular Formula	C26H24FN5O2S
MDL Number	MFCD32671350
Molecular Weight	489.56
MOL File	1252765-13-1.mol

Chemical Properties

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
InChIKey	IVOACCSOISMVBL-UHFFFAOYSA-N
SMILES	C(N1CCN(C2CN(C(C3C=CC4=C(C=3)C=CN4C3=CC=C(F)C=C3)=O)C2)CC1)(C1=NC=CS1)=O

Hazard Information

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 t_1/2 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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