SML0872
MJN110
≥98% (HPLC)
别名:
2,5-dioxopyrrolidin-1-yl 4-(bis(4-chlorophenyl)methyl)piperazine-1-carboxylate, Cravatt Reagent
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关于此项目
经验公式（希尔记法）:
C22H21Cl2N3O4
化学文摘社编号:
分子量:
462.33
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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 string
O=C(ON1C(CCC1=O)=O)N2CCN(C(C3=CC=C(Cl)C=C3)C4=CC=C(Cl)C=C4)CC2
InChI key
BEADRWVIFHOSGN-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
room temp
Quality Level
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Application
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.
Biochem/physiol Actions
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.
Features and Benefits
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.
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Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
Lipid droplet-dependent fatty acid metabolism controls the immune suppressive phenotype of tumor-associated macrophages
Wu H, et al.
EMBO Molecular Medicine (2019)
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+
Elizabeth A Fucich et al.
Journal of neurophysiology, 123(2), 707-717 (2020-01-09)
Our previous work showed that lateral fluid percussion injury to the sensorimotor cortex (SMC) of anesthetized rats increased neuronal synaptic hyperexcitability in layer 5 (L5) neurons in ex vivo brain slices 10 days postinjury. Furthermore, endocannabinoid (EC) degradation inhibition via
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