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MJN110

Cat. No. M8414
MJN110 Structure
Size Price Availability
10mg USD 90  USD90 4-7 Days
50mg USD 320  USD320 4-7 Days
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Biological Activity

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.

Chemical Information
Molecular Weight 462.33
Formula C22H21Cl2N3O4
CAS Number 1438416-21-7
Solubility (25°C) DMSO: 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Prabhuanand Selvaraj, et al. The Novel Monoacylglycerol Lipase Inhibitor MJN110 Suppresses Neuroinflammation, Normalizes Synaptic Composition and Improves Behavioral Performance in the Repetitive Traumatic Brain Injury Mouse Model

[2] Alexis F League, et al. Monoacylglycerol Lipase Inhibitor MJN110 Reduces Neuronal Hyperexcitability, Restores Dendritic Arborization Complexity, and Regulates Reward-Related Behavior in Presence of HIV-1 Tat

[3] Malte Feja, et al. The novel MAGL inhibitor MJN110 enhances responding to reward-predictive incentive cues by activation of CB1 receptors

[4] Stephen G Woodhams, et al. The cannabinoid system and pain

[5] Jenny L Wilkerson, et al. The Selective Monoacylglycerol Lipase Inhibitor MJN110 Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model

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Keywords: MJN110 supplier, MAGL, inhibitors, activators

 
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