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MedKoo Cat#: 555192 | Name: MJN-110
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

MJN110 is a potent and selective MAGL inhibitor. MJN110 inhibits MAGL (IC50 = 9.1 nM). MJN110 Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model.

Chemical Structure

MJN-110
MJN-110
CAS#1438416-21-7

Theoretical Analysis

MedKoo Cat#: 555192

Name: MJN-110

CAS#: 1438416-21-7

Chemical Formula: C22H21Cl2N3O4

Exact Mass: 461.0909

Molecular Weight: 462.33

Elemental Analysis: C, 57.15; H, 4.58; Cl, 15.34; N, 9.09; O, 13.84

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 weeks
25mg USD 650.00 2 weeks
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Related CAS #
No Data
Synonym
MJN-110; MJN 110; MJN110.
IUPAC/Chemical Name
4-[bis(4-chlorophenyl)methyl]-1-piperazinecarboxylic acid, 2,5-dioxo-1-pyrrolidinyl ester
InChi Key
BEADRWVIFHOSGN-UHFFFAOYSA-N
InChi Code
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
SMILES Code
O=C(N1CCN(C(C2=CC=C(Cl)C=C2)C3=CC=C(Cl)C=C3)CC1)ON4C(CCC4=O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
MJN110 is a monoacylglycerol lipase (MAGL) inhibitor with IC50s of 9.1 nM and 2.1 nM for hMAGL and 2-arachidonoylglycerol (2-AG).
In vitro activity:
This study treated PC3 cells, a human prostate cancer cell line that expresses both MAGL and ABHD6, with MJN110 (0.01–1000 nM, 4 h) and then harvested cells and analyzed their proteomes by gel-based competitive ABPP with FP-Rh. This study identified hMAGL as the primary serine hydrolase target of MJN110 with an IC50 of ∼1 nM and 10- and 100-fold selectivity windows over ABHD6 and LYPLA1/2, respectively (Figure 5E). Reference: ACS Chem Neurosci. 2013 Sep 18;4(9):1322-32. https://pubmed.ncbi.nlm.nih.gov/23731016/
In vivo activity:
Administration of MJN110 selectively elevated the levels of 2-AG and reduced the production of arachidonic acid (AA) and prostaglandin E2 (PGE2) in the TBI mouse brain. The increased production of proinflammatory cytokines, accumulation of astrocytes and microglia in the TBI mouse ipsilateral cerebral cortex and hippocampus were significantly reduced by MJN110 treatment. MJN110 treatment normalized the expression of the NMDA receptor subunits NR2A and NR2B, the AMPA receptor subunits GluR1 and GluR2, and the GABAA receptor subunits α1, β2,3 and γ2, which were all reduced at 1, 2 and 4 weeks post-injury. Reference: Cells. 2021 Dec 8;10(12):3454. https://pubmed.ncbi.nlm.nih.gov/34943962/
Solvent mg/mL mM comments
Solubility
DMF 25.0 54.07
DMSO 140.0 302.82
Ethanol 0.3 0.54
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 462.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. League AF, Gorman BL, Hermes DJ, Johnson CT, Jacobs IR, Yadav-Samudrala BJ, Poklis JL, Niphakis MJ, Cravatt BF, Lichtman AH, Ignatowska-Jankowska BM, Fitting S. Monoacylglycerol Lipase Inhibitor MJN110 Reduces Neuronal Hyperexcitability, Restores Dendritic Arborization Complexity, and Regulates Reward-Related Behavior in Presence of HIV-1 Tat. Front Neurol. 2021 Aug 16;12:651272. doi: 10.3389/fneur.2021.651272. PMID: 34484091; PMCID: PMC8415271. 2. Niphakis MJ, Cognetta AB 3rd, Chang JW, Buczynski MW, Parsons LH, Byrne F, Burston JJ, Chapman V, Cravatt BF. Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors. ACS Chem Neurosci. 2013 Sep 18;4(9):1322-32. doi: 10.1021/cn400116z. Epub 2013 Jun 17. PMID: 23731016; PMCID: PMC3778430. 3. Selvaraj P, Tanaka M, Wen J, Zhang Y. The Novel Monoacylglycerol Lipase Inhibitor MJN110 Suppresses Neuroinflammation, Normalizes Synaptic Composition and Improves Behavioral Performance in the Repetitive Traumatic Brain Injury Mouse Model. Cells. 2021 Dec 8;10(12):3454. doi: 10.3390/cells10123454. PMID: 34943962; PMCID: PMC8700188. 4. Diester CM, Lichtman AH, Negus SS. Behavioral Battery for Testing Candidate Analgesics in Mice. II. Effects of Endocannabinoid Catabolic Enzyme Inhibitors and ∆9-Tetrahydrocannabinol. J Pharmacol Exp Ther. 2021 May;377(2):242-253. doi: 10.1124/jpet.121.000497. Epub 2021 Feb 23. PMID: 33622769; PMCID: PMC8058502.
In vitro protocol:
1. League AF, Gorman BL, Hermes DJ, Johnson CT, Jacobs IR, Yadav-Samudrala BJ, Poklis JL, Niphakis MJ, Cravatt BF, Lichtman AH, Ignatowska-Jankowska BM, Fitting S. Monoacylglycerol Lipase Inhibitor MJN110 Reduces Neuronal Hyperexcitability, Restores Dendritic Arborization Complexity, and Regulates Reward-Related Behavior in Presence of HIV-1 Tat. Front Neurol. 2021 Aug 16;12:651272. doi: 10.3389/fneur.2021.651272. PMID: 34484091; PMCID: PMC8415271. 2. Niphakis MJ, Cognetta AB 3rd, Chang JW, Buczynski MW, Parsons LH, Byrne F, Burston JJ, Chapman V, Cravatt BF. Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors. ACS Chem Neurosci. 2013 Sep 18;4(9):1322-32. doi: 10.1021/cn400116z. Epub 2013 Jun 17. PMID: 23731016; PMCID: PMC3778430.
In vivo protocol:
1. Selvaraj P, Tanaka M, Wen J, Zhang Y. The Novel Monoacylglycerol Lipase Inhibitor MJN110 Suppresses Neuroinflammation, Normalizes Synaptic Composition and Improves Behavioral Performance in the Repetitive Traumatic Brain Injury Mouse Model. Cells. 2021 Dec 8;10(12):3454. doi: 10.3390/cells10123454. PMID: 34943962; PMCID: PMC8700188. 2. Diester CM, Lichtman AH, Negus SS. Behavioral Battery for Testing Candidate Analgesics in Mice. II. Effects of Endocannabinoid Catabolic Enzyme Inhibitors and ∆9-Tetrahydrocannabinol. J Pharmacol Exp Ther. 2021 May;377(2):242-253. doi: 10.1124/jpet.121.000497. Epub 2021 Feb 23. PMID: 33622769; PMCID: PMC8058502.
1: Choi SH, Arai AL, Mou Y, Kang B, Yen CC, Hallenbeck J, Silva AC. Neuroprotective Effects of MAGL (Monoacylglycerol Lipase) Inhibitors in Experimental Ischemic Stroke. Stroke. 2018 Mar;49(3):718-726. doi: 10.1161/STROKEAHA.117.019664. Epub 2018 Feb 13. PubMed PMID: 29440474; PubMed Central PMCID: PMC5829008. 2: Fontenot J, Loetz EC, Ishiki M, Bland ST. Monoacylglycerol lipase inhibition alters social behavior in male and female rats after post-weaning social isolation. Behav Brain Res. 2018 Apr 2;341:146-153. doi: 10.1016/j.bbr.2017.12.038. Epub 2017 Dec 29. PubMed PMID: 29292159. 3: Flannery LE, Henry RJ, Kerr DM, Finn DP, Roche M. FAAH, but not MAGL, inhibition modulates acute TLR3-induced neuroimmune signaling in the rat, independent of sex. J Neurosci Res. 2017 Jul 20. doi: 10.1002/jnr.24120. [Epub ahead of print] PubMed PMID: 28726298. 4: Wills KL, DeVuono MV, Limebeer CL, Vemuri K, Makriyannis A, Parker LA. CB₁ receptor antagonism in the bed nucleus of the stria terminalis interferes with affective opioid withdrawal in rats. Behav Neurosci. 2017 Aug;131(4):304-11. doi: 10.1037/bne0000201. PubMed PMID: 28714716. 5: Owens RA, Mustafa MA, Ignatowska-Jankowska BM, Damaj MI, Beardsley PM, Wiley JL, Niphakis MJ, Cravatt BF, Lichtman AH. Inhibition of the endocannabinoid-regulating enzyme monoacylglycerol lipase elicits a CB(1) receptor-mediated discriminative stimulus in mice. Neuropharmacology. 2017 Oct;125:80-86. doi: 10.1016/j.neuropharm.2017.06.032. Epub 2017 Jun 30. PubMed PMID: 28673548; PubMed Central PMCID: PMC5771234. 6: Woodhams SG, Chapman V, Finn DP, Hohmann AG, Neugebauer V. The cannabinoid system and pain. Neuropharmacology. 2017 Sep 15;124:105-120. doi: 10.1016/j.neuropharm.2017.06.015. Epub 2017 Jun 15. Review. PubMed PMID: 28625720; PubMed Central PMCID: PMC5785108. 7: Ahamed M, Attili B, van Veghel D, Ooms M, Berben P, Celen S, Koole M, Declercq L, Savinainen JR, Laitinen JT, Verbruggen A, Bormans G. Synthesis and preclinical evaluation of [(11)C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL). Eur J Med Chem. 2017 Aug 18;136:104-113. doi: 10.1016/j.ejmech.2017.04.066. Epub 2017 Apr 25. PubMed PMID: 28486208. 8: Burston JJ, Mapp PI, Sarmad S, Barrett DA, Niphakis MJ, Cravatt BF, Walsh DA, Chapman V. Robust anti-nociceptive effects of monoacylglycerol lipase inhibition in a model of osteoarthritis pain. Br J Pharmacol. 2016 Nov;173(21):3134-3144. doi: 10.1111/bph.13574. Epub 2016 Sep 23. PubMed PMID: 27501482; PubMed Central PMCID: PMC5056226. 9: Owens RA, Ignatowska-Jankowska B, Mustafa M, Beardsley PM, Wiley JL, Jali A, Selley DE, Niphakis MJ, Cravatt BF, Lichtman AH. Discriminative Stimulus Properties of the Endocannabinoid Catabolic Enzyme Inhibitor SA-57 in Mice. J Pharmacol Exp Ther. 2016 Aug;358(2):306-14. doi: 10.1124/jpet.115.229492. Epub 2016 Jun 15. PubMed PMID: 27307500; PubMed Central PMCID: PMC4959103. 10: Limebeer CL, Rock EM, Puvanenthirarajah N, Niphakis MJ, Cravatt BF, Parker LA. Elevation of 2-AG by monoacylglycerol lipase inhibition in the visceral insular cortex interferes with anticipatory nausea in a rat model. Behav Neurosci. 2016 Apr;130(2):261-6. doi: 10.1037/bne0000132. PubMed PMID: 26974857; PubMed Central PMCID: PMC4793281. 11: Berdan CA, Erion KA, Burritt NE, Corkey BE, Deeney JT. Inhibition of Monoacylglycerol Lipase Activity Decreases Glucose-Stimulated Insulin Secretion in INS-1 (832/13) Cells and Rat Islets. PLoS One. 2016 Feb 11;11(2):e0149008. doi: 10.1371/journal.pone.0149008. eCollection 2016. PubMed PMID: 26867016; PubMed Central PMCID: PMC4750965. 12: Wilkerson JL, Niphakis MJ, Grim TW, Mustafa MA, Abdullah RA, Poklis JL, Dewey WL, Akbarali H, Banks ML, Wise LE, Cravatt BF, Lichtman AH. 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. doi: 10.1124/jpet.115.229971. Epub 2016 Jan 20. PubMed PMID: 26791602; PubMed Central PMCID: PMC4809319. 13: Wills KL, Petrie GN, Millett G, Limebeer CL, Rock EM, Niphakis MJ, Cravatt BF, Parker LA. Double Dissociation of Monoacylglycerol Lipase Inhibition and CB1 Antagonism in the Central Amygdala, Basolateral Amygdala, and the Interoceptive Insular Cortex on the Affective Properties of Acute Naloxone-Precipitated Morphine Withdrawal in Rats. Neuropsychopharmacology. 2016 Jun;41(7):1865-73. doi: 10.1038/npp.2015.356. Epub 2015 Dec 9. PubMed PMID: 26647976; PubMed Central PMCID: PMC4869055. 14: Sticht MA, Limebeer CL, Rafla BR, Abdullah RA, Poklis JL, Ho W, Niphakis MJ, Cravatt BF, Sharkey KA, Lichtman AH, Parker LA. Endocannabinoid regulation of nausea is mediated by 2-arachidonoylglycerol (2-AG) in the rat visceral insular cortex. Neuropharmacology. 2016 Mar;102:92-102. doi: 10.1016/j.neuropharm.2015.10.039. Epub 2015 Nov 2. PubMed PMID: 26541329; PubMed Central PMCID: PMC4698202. 15: Ignatowska-Jankowska B, Wilkerson JL, Mustafa M, Abdullah R, Niphakis M, Wiley JL, Cravatt BF, Lichtman AH. Selective monoacylglycerol lipase inhibitors: antinociceptive versus cannabimimetic effects in mice. J Pharmacol Exp Ther. 2015 May;353(2):424-32. doi: 10.1124/jpet.114.222315. Epub 2015 Mar 11. PubMed PMID: 25762694; PubMed Central PMCID: PMC4407719. 16: Parker LA, Niphakis MJ, Downey R, Limebeer CL, Rock EM, Sticht MA, Morris H, Abdullah RA, Lichtman AH, Cravatt BF. 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. doi: 10.1007/s00213-014-3696-x. Epub 2014 Aug 3. PubMed PMID: 25085768. 17: Niphakis MJ, Cognetta AB 3rd, Chang JW, Buczynski MW, Parsons LH, Byrne F, Burston JJ, Chapman V, Cravatt BF. Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors. ACS Chem Neurosci. 2013 Sep 18;4(9):1322-32. doi: 10.1021/cn400116z. Epub 2013 Jun 17. PubMed PMID: 23731016; PubMed Central PMCID: PMC3778430.

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MK-0354