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MAGLi 432

Cat. No. M21099
MAGLi 432 Structure
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Biological Activity

MAGLi 432 is a novel, reversible inhibitor of monoacylglycerol lipase (MAGL). MAGLi 432 binds with high affinity to the MAGL active site with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme).

Chemical Information
Molecular Weight 463.80
Formula C22H24BrClN2O2
CAS Number 2361575-20-2
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] Alicia M Kemble, et al. PLoS One. A potent and selective inhibitor for the modulation of MAGL activity in the neurovasculature

[2] Beatrice Severino, et al. Front Pharmacol. Development, Validation of LC-MS/MS Method and Determination of Pharmacokinetic Parameters of the Stroke Neuroprotectant Neurounina-1 in Beagle Dog Plasma After Intravenous Administration

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  Catalog
Abmole Inhibitor Catalog




Keywords: MAGLi 432 supplier, MAGL, inhibitors, activators


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