MJN110
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 462.3 |
Cas No. | 1438416-21-7 |
Formula | C22H21Cl2N3O4 |
Synonyms | 2,5-Dioxopyrrolidin-1-yl 4-[bis(4-chlorophenyl)methyl]piperazine-1-carboxylate |
Solubility | insoluble in EtOH; insoluble in H2O; ≥49.3 mg/mL in DMSO |
Chemical Name | 4-[bis(4-chlorophenyl)methyl]-1-piperazinecarboxylic acid, 2,5-dioxo-1-pyrrolidinyl ester |
SDF | Download SDF |
Canonical SMILES | ClC1=CC=C(C(C2=CC=C(Cl)C=C2)N3CCN(C(ON4C(CCC4=O)=O)=O)CC3)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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