MJN110 (Synonyms: 2,5-Dioxopyrrolidin-1-yl 4-[bis(4-chlorophenyl)methyl]piperazine-1-carboxylate) |
| Catalog No.GC14079 |
MJN110은 경구 활성 및 선택적 모노아실글리세롤 리파제(MAGL) 억제제로 IC50이 hMAGL 및 2-AG에 대해 각각 9.1nM 및 2.1nM입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1438416-21-7
Sample solution is provided at 25 µL, 10mM.
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Targets: MAGL
IC50: 9.1 nM
MJN110 is an N-hydroxysuccinimidyl carbamate with great, selective, and in-vivo-active inhibition effect for monoacylglycerol lipase (MAGL) with the IC50 value of 9.1 nM. Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) are biologically active lipids which participate in a mount of synaptic processes. MAGL is a serine hydrolase in charge of the hydrolysis of 2-AG to glycerol and arachidonic acid to terminate its function. And MJN110 could significantly inhibit the hydrolysis of 2-AG with the IC50 value of 2.1 nM without any effect on the hydrolysis of AEA up to 50 μM [1].
In Vitro: In HEK293T cells, MJN110 could inactivate hMAGL with the IC50 value of 9.1 nM, while having no effect on hFAAH activity. Besides, in human prostate cancer cell line PC3 cells which express both MAGL and ABDH6, MJN110 could selectively inhibit MAGL with the IC50 value of ~1 nM and 10-fold over ABDH6 [1].
In Vivo: In a rat model of Diabetic Neuropathy, administrator of MJN110 (5.0 mg·kg-1, i.p.) could alleviate mechanical allodynia by significantly increasing mechanical withdrawal thresholds [1]. Besides, in the mouse chronic constriction injury (CCI) of the sciatic nerve model of neuropathic pain, i.p. administration of MJN110 combined with morphine (the ED50 values of 0.43 mg/kg and 2.4 mg/kg, respectively) could produce opioid-sparing effects with diminished tolerance and cannabimimetic side effects [2].
Clinical trial: No data available.
References:
[1] Niphakis M J, Cognetta A B, Chang J W, et al. Evaluation of NHS carbamates as a potent and selective class of endocannabinoid hydrolase inhibitors.[J]. ACS Chemical Neuroscience, 2013, 4(9): 1322-1332.
[2] Wilkerson J L, Niphakis M J, Grim T W, et al. The selective monoacylglycerol lipase inhibitor MJN110 produces opioid sparing effects in a mouse neuropathic pain model[J]. Journal of Pharmacology and Experimental Therapeutics, 2016, 357(1): 145-156.
| Cas No. | 1438416-21-7 | SDF | |
| Synonyms | 2,5-Dioxopyrrolidin-1-yl 4-[bis(4-chlorophenyl)methyl]piperazine-1-carboxylate | ||
| Chemical Name | 4-[bis(4-chlorophenyl)methyl]-1-piperazinecarboxylic acid, 2,5-dioxo-1-pyrrolidinyl ester | ||
| Canonical SMILES | ClC1=CC=C(C(C2=CC=C(Cl)C=C2)N3CCN(C(ON4C(CCC4=O)=O)=O)CC3)C=C1 | ||
| Formula | C22H21Cl2N3O4 | M.Wt | 462.3 |
| Solubility | ≤0.25mg/ml in ethanol;30mg/ml in DMSO;25mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1631 mL | 10.8155 mL | 21.631 mL |
| 5 mM | 0.4326 mL | 2.1631 mL | 4.3262 mL |
| 10 mM | 0.2163 mL | 1.0815 mL | 2.1631 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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