| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
MJN-110 targets monoacylglycerol lipase (MAGL), the primary enzyme responsible for degrading the endocannabinoid 2-arachidonoylglycerol (2-AG). By inhibiting MAGL, MJN-110 increases the levels of 2-AG, which activates cannabinoid receptors CB1 and CB2, leading to analgesic and anti-inflammatory effects. Its high selectivity for MAGL over FAAH ensures that it does not affect anandamide levels, providing a more targeted modulation of the endocannabinoid system.
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| ln Vitro |
The main target of serine hydrolase, hMAGL, is MJN110 (0.01-1000 nM; 4 hours); its IC50 is about 1 nM, and its selectivity window is 10- and 100-fold greater than that of ABHD6 and LYPLA1/2, respectively [2].
In vitro, MJN-110 potently inhibits hMAGL with an IC50 of 9.1 nM and inhibits 2-AG hydrolysis with an IC50 of 2.1 nM. It exhibits over 10,000-fold selectivity for MAGL over FAAH. These in vitro activities confirm its mechanism as a selective MAGL inhibitor. |
| ln Vivo |
In a dose-dependent manner, MJN110 (ip; 0.0818 mg/kg; twice daily for 5.5 days) reverses the effects of chronic constriction injury (CCI) on mechanical allodynia and thermal hyperalgesia. 0.430 (0.233-0.793) mg/kg is the comparable ED50 value (95% confidence limit)[1].
In vivo, MJN-110 is orally active and produces opioid-like protective effects. It has strong anti-hyperalgesic activity, making it a valuable tool for studying pain modulation. Its ability to increase 2-AG levels in the brain contributes to its analgesic effects. |
| Enzyme Assay |
The in vitro enzyme inhibition assay for MJN-110 involves measuring MAGL activity using a fluorogenic or radiolabeled substrate. The enzyme is incubated with the compound, and the hydrolysis product is quantified. The IC50 is determined from dose-response curves.
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| Cell Assay |
Western blot analysis[2]
Cell Types: Human PC3 cells Tested Concentrations: 0.01, 0.1, 1, 10, 100, 1000 nM Incubation Duration: 4 hrs (hours) Experimental Results: HMAGL acts as a major serine hydrolase target with an IC50 of approximately 1 nM. Cellular assays for MJN-110 involve treating cells with the compound and measuring the levels of 2-AG and other endocannabinoids. The inhibition of MAGL activity is confirmed by the accumulation of 2-AG. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice, body weight range 18 to 35 g[1]
Doses: 0.0818 mg/kg Route of Administration: intraperitoneal (ip) injection; twice (two times) daily for 5.5 days Experimental Results: Reversal of CCI-induced disease in a dose-dependent manner of mechanical allodynia and thermal hyperalgesia. In vivo efficacy of MJN-110 is evaluated in animal models of pain, such as the formalin test or neuropathic pain models. The compound is administered orally, and pain responses are measured. |
| ADME/Pharmacokinetics |
MJN-110 has a molecular weight of 462.33 g/mol and a molecular formula of C22H21Cl2N3O4. It is orally bioavailable.
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| Toxicity/Toxicokinetics |
The toxicity profile of MJN-110 is limited. As a research-grade compound, comprehensive toxicological evaluations have not been published.
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| References |
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| Additional Infomation |
MJN110 is a diarylmethane.
MJN-110 is a research compound for studying the endocannabinoid system and pain modulation. It has not entered clinical trials. Its mechanism involves potent and selective inhibition of MAGL. |
| Molecular Formula |
C22H21CL2N3O4
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|---|---|
| Molecular Weight |
462.327
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| Exact Mass |
461.091
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| CAS # |
1438416-21-7
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| PubChem CID |
71722059
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| Appearance |
White to off-white solid powder
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| Density |
1.47±0.1 g/cm3
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| Boiling Point |
561.5±60.0 °C
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| LogP |
3.714
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
632
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BEADRWVIFHOSGN-UHFFFAOYSA-N
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| 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
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 4-[bis(4-chlorophenyl)methyl]piperazine-1-carboxylate
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| Synonyms |
MJN110; MJN 110; MJN-110
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~540.74 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1630 mL | 10.8148 mL | 21.6296 mL | |
| 5 mM | 0.4326 mL | 2.1630 mL | 4.3259 mL | |
| 10 mM | 0.2163 mL | 1.0815 mL | 2.1630 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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