MJN110

Names

[ Name ]:
MJN110

[Synonym ]:
MJN110
2,5-dioxopyrrolidin-1-yl 4-[bis(4-chlorophenyl)methyl]piperazine-1-carboxylate

Biological Activity

[Description]:

MJN110 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor[1]. MJN110 reduces hepatic macrophage number, inflammatory gene expression and slowes down fibrosis progression[2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> MAGL

Research Areas >> Inflammation/Immunology

[In Vivo]

MJN110 (i.p.; 0.0818 mg/kg; twice daily for 5.5 days) reverses chronic constriction injury (CCI)-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner. The respective ED50 value (95% confidence limits) is 0.430 (0.233-0.793) mg/kg[1]. Animal Model: Male C57BL/6J mice ranged from 18 to 35 g[1] Dosage: 0.0818 mg/kg Administration: I.p.; twice daily for 5.5 days Result: Reversed CCI-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner.

[References]

[1]. Wilkerson JL, et al. The Selective Monoacylglycerol Lipase Inhibitor MJN110 Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model. J Pharmacol Exp Ther. 2016 Apr;357(1):145-56.

[2]. Habib A, et al. Inhibition of monoacylglycerol lipase, an anti-inflammatory and antifibrogenic strategy in the liver. Gut. 2018 Oct 9. pii: gutjnl-2018-316137.

Chemical & Physical Properties

[ Density]:
1.47±0.1 g/cm3

[ Boiling Point ]:
561.5±60.0 °C

[ Molecular Formula ]:
C₂₂H₂₁Cl₂N₃O₄

[ Molecular Weight ]:
462.32600

[ Exact Mass ]:
461.09100

[ PSA ]:
70.16000

[ LogP ]:
3.71470

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Hazard Codes ]:
Xi

[ Risk Phrases ]:
22-50/53

[ Safety Phrases ]:
26-60-61

[ RIDADR ]:
NONH for all modes of transport

Articles

Effect of selective inhibition of monoacylglycerol lipase (MAGL) on acute nausea, anticipatory nausea, and vomiting in rats and Suncus murinus.

Psychopharmacol. Ser. 232(3) , 583-93, (2015)

To determine the role of the endocannabinoid, 2-arachodonyl glycerol (2-AG), in the regulation of nausea and vomiting.We evaluated the effectiveness of the potent selective monoacylglycerol lipase (MA...

Proteome-wide reactivity profiling identifies diverse carbamate chemotypes tuned for serine hydrolase inhibition.

ACS Chem. Biol. , (2013)

Serine hydrolases are one of the largest and most diverse enzyme classes in Nature. Inhibitors of serine hydrolases are used to treat many diseases, including obesity, diabetes, cognitive dementia, an...

Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors.

ACS Chem. Neurosci. 4(9) , 1322-32, (2013)

Monoacylglycerol lipase (MAGL) is a principal metabolic enzyme responsible for hydrolyzing the endogenous cannabinoid (endocannabinoid) 2-arachidonoylglycerol (2-AG). Selective inhibitors of MAGL offe...