SML0872

MJN110

≥98% (HPLC)

• Synonyme(s) : 2,5-dioxopyrrolidin-1-yl 4-(bis(4-chlorophenyl)methyl)piperazine-1-carboxylate, Cravatt Reagent
• Formule empirique (notation de Hill) : C₂₂H₂₁Cl₂N₃O₄
• CAS Number: 1438416-21-7
• Poids moléculaire : 462.33
• Numéro MDL: MFCD26960823
• Code UNSPSC : 12352200
• ID de substance PubChem : 329825611
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 20 mg/mL, clear
• Température de stockage: room temp
• Chaîne SMILES: 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
• Clé InChI: BEADRWVIFHOSGN-UHFFFAOYSA-N

Description

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.

Actions biochimiques/physiologiques

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.

Caractéristiques et avantages

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Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H302
• Conseils de prudence: P264 - P270 - P301 + P312 - P501
• Classification des risques: Acute Tox. 4 Oral
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable