| Identification | Back Directory | [Name]
Cravatt Reagent | [CAS]
1438416-21-7 | [Synonyms]
KT172
HT-01
KT195
KT109
MJN110
Cravatt Reagent
MJN110 >=98% (HPLC)
BEADRWVIFHOSGN-UHFFFAOYSA-N
MAGL,MJN 110,Inhibitor,Monoacylglycerol lipase,MJN110,MJN-110,inhibit
2,5-dioxopyrrolidin-1-yl 4-(bis(4-chlorophenyl)methyl)piperazine-1-carboxylate
(4-([1,1′-Biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)(2-benzylpiperidin-1-yl)methanone
1-Piperazinecarboxylic acid, 4-[bis(4-chlorophenyl)methyl]-, 2,5-dioxo-1-pyrrolidinyl ester
(2-Benzylpiperidin-1-yl)(4-(2′-methoxy-[1,1′-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)methanone
N-(5-(3-(5,5-Difluoro-7,9-dimethyl-5H-4l4,5l4-dipyrrolo[1,2-c:2′,1′-f][1,3,2]diazaborinin-3-yl)propanamido)pentyl)-N-phenethyl-4-(4-(trifluoromethoxy)phenyl)-1H-1,2,3-triazole-1-carboxamide | [Molecular Formula]
C22H21Cl2N3O4 | [MDL Number]
MFCD26960823 | [MOL File]
1438416-21-7.mol | [Molecular Weight]
462.33 |
| Chemical Properties | Back Directory | [Boiling point ]
561.5±60.0 °C(Predicted) | [density ]
1.47±0.1 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO: soluble20mg/mL, clear | [form ]
powder | [pka]
5.07±0.10(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
Endocannabinoids such as 2-arachidonoyl glycerol (2-AG; ) and arachidonoyl ethanolamide (AEA; ) are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to arachidonic acid and glycerol, thus terminating its biological function. MJN110 is an N-hydroxysuccinimidyl carbamate that inhibits MAGL (IC50 = 9.1 nM) and to a lesser extent ABHD6 with potent selectivity over FAAH (IC50 > 10 μM) and other brain serine hydrolases. It can inhibit 2-AG hydrolysis (IC50 = 2.1 nM) with no effect on AEA hydrolysis up to 50 μM. At 5 mg/kg, MJN110 has been shown to alleviate mechanical allodynia in a rat model of diabetic neuropathy.[Cayman Chemical] | [Uses]
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. | [in vivo]
MJN110 (i.p.; 0.0818 mg/kg; twice daily for 5.5 days) reverses chronic constriction injury (CCI)-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner. The respective ED50 value (95% confidence limits) is 0.430 (0.233-0.793) mg/kg[1]. | Animal Model: | Male C57BL/6J mice ranged from 18 to 35 g[1] | | Dosage: | 0.0818 mg/kg | | Administration: | I.p.; twice daily for 5.5 days | | Result: | Reversed CCI-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner.
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