For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I011653 |
| CAS Number | 1438416-21-7 |
| Synonyms | (2,5-dioxopyrrolidin-1-yl) 4-[bis(4-chlorophenyl)methyl]piperazine-1-carboxylate |
| Molecular Formula | C22H21Cl2N3O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H21Cl2N3O4/c23-17-5-1-15(2-6-17)21(16-3-7-18(24)8-4-16)25-11-13-26(14-12-25)22(30)31-27-19(28)9-10-20(27)29/h1-8,21H,9-14H2 |
| InChIKey | BEADRWVIFHOSGN-UHFFFAOYSA-N |
| SMILES | C1CC(=O)N(C1=O)OC(=O)N2CCN(CC2)C(C3=CC=C(C=C3)Cl)C4=CC=C(C=C4)Cl |
| 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. |
