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MJN110
Axon 2580
CAS:
1438416-21-7
Purity:
98%
- Soluble in DMSO
- MF: C22H21Cl2N3O4
- MW: 462.33
Description
Potent, selective, and in-vivo-active MAGL inhibitor (IC50 values 9.5 nM and 260 nM for inhibition of mouse MAGL and ABHD6, respectively) displaying strong antihyperalgesic activity (mechanical allodynia) in a rat model of diabetic neuropathy. MJN110 exhibits therapeutic potential in the treatment of acute nausea and vomiting as well as anticipatory nausea by elevation of endogenous cannabinoid 2-arachidonoylglycerol (2-AG) levels in the brain.
More Information
| Parent CAS No. | 1438416-21-7 |
|---|---|
| Chemical Name | 2,5-dioxopyrrolidin-1-yl 4-(bis(4-chlorophenyl)methyl)piperazine-1-carboxylate |
| SMILES | N1(C(ON2C(=O)CCC2=O)=O)CCN(C(C2=CC=C(Cl)C=C2)C2=CC=C(Cl)C=C2)CC1 |
| MFCD | N.A. |
| 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 |
| CID | 71722059 |
| Short Description | MAGL inhibitor |
References
- B Ignatowska-Jankowska et al. Selective monoacylglycerol lipase inhibitors: antinociceptive versus cannabimimetic effects in mice. J Pharmacol Exp Ther. 2015 May;353(2):424-32.
- MJ Niphakis 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.
- LA Parker et al. Effect of selective inhibition of monoacylglycerol lipase (MAGL) on acute nausea, anticipatory nausea, and vomiting in rats and Suncus murinus. Psychopharmacology (Berl). 2015 Feb;232(3):583-93.
- JW Chang et al. Proteome-wide reactivity profiling identifies diverse carbamate chemotypes tuned for serine hydrolase inhibition. ACS Chem Biol. 2013 Jul 19;8(7):1590-9.
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