MJN110_product_DataBase

Bioactivity

MJN110 is an orally active and selective monoacylglycerol lipase (MAGL) inhibitor with IC50s of 9.1 nM and 2.1 nM for hMAGL and 2-arachidonoylglycerol (2-AG), respectively[1]. MJN110 produces opioid-sparing effects and displays strong antihyperalgesic activity[2].

Target

IC50: 9.1 nM (hMAGL) and 2.1 nM (2-AG)

Invitro

MJN110 (0.01-1000 nM; 4 hours) has the primary serine hydrolase target, hMAGL, with an IC50 of ~1 nM and 10- and 100-fold selectivity windows over ABHD6 and LYPLA1/2, respectively[2]. Western Blot Analysis[2] Cell Line:

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:

Name

MJN110

CAS

1438416-21-7

Formula

C22H21Cl2N3O4

Molar Mass

462.33

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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]. Niphakis MJ, et al. Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors. ACS Chem Neurosci. 2013 Sep 18;4(9):1322-32.

PeptideDB

MJN110

CAS: 1438416-21-7 F: C22H21Cl2N3O4 W: 462.33