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Merck
CN

SML0872

Sigma-Aldrich

MJN110

≥98% (HPLC)

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别名:
2,5-dioxopyrrolidin-1-yl 4-(bis(4-chlorophenyl)methyl)piperazine-1-carboxylate, Cravatt Reagent
经验公式(希尔记法):
C22H21Cl2N3O4
分子量:
462.33
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 20 mg/mL, clear

储存温度

room temp

SMILES字符串

O=C(ON1C(CCC1=O)=O)N2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=C(Cl)C=C4)CC2

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

InChI key

BEADRWVIFHOSGN-UHFFFAOYSA-N

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相关类别

应用

MJN110 has been used as a monoacylglycerol lipase (MAGL) inhibitor to study its effect on aggressive grooming in rats. It has also been used to inhibit lipid droplet formation.

生化/生理作用

MJN110 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) with >10,000 selectivity over FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA). MJN110 inhibits rat, mouse and human MAGL with IC50 values ranging from < 100 nM in rat to an IC50 of ~1 nM with 10- and 100-fold selectivity over closely related ABHD6, a serine hydrolase that acts as an alternative hydrolase of 2-AG, and LYPLA1/2 in human PC3 cells. MJN110 showed potent anti-hyperalgesic activity in a rat model of diabetic neuropathy, showing a therapeutic potential for treating diabetes chronic pain.

特点和优势

This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

象形图

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警示用语:

Warning

危险声明

危险分类

Acute Tox. 4 Oral

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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Monoacylglycerol lipase inhibition alters social behavior in male and female rats after post-weaning social isolation
Fontenot J, et al.
Behavioural Brain Research, 341, 146-153 (2018)
Lipid droplet-dependent fatty acid metabolism controls the immune suppressive phenotype of tumor-associated macrophages
Wu H, et al.
EMBO Molecular Medicine (2019)
Robert A Owens et al.
Neuropharmacology, 125, 80-86 (2017-07-05)
Substantial challenges exist for investigating the cannabinoid receptor type 1 (CB
A L Thompson et al.
The Journal of pharmacology and experimental therapeutics, 373(2), 230-238 (2020-02-15)
Metastatic breast cancer is prevalent worldwide, and one of the most common sites of metastasis is long bones. Of patients with disease, the major symptom is pain, yet current medications fail to adequately result in analgesic efficacy and present major
Jae Won Chang et al.
ACS chemical biology, 8(7), 1590-1599 (2013-05-25)
Serine hydrolases are one of the largest and most diverse enzyme classes in Nature. Inhibitors of serine hydrolases are used to treat many diseases, including obesity, diabetes, cognitive dementia, and bacterial and viral infections. Nonetheless, the majority of the 200+

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