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MAGLi 432

Chemical Structure : MAGLi 432

CAS No.: 2361576-42-1

MAGLi 432 (MAGLi432)

Catalog No.: PC-49167Not For Human Use, Lab Use Only.

MAGLi 432 is a highly selective, potent and reversible monoacylglycerol lipase (MAGL) inhibitor with IC50 of 4.2 and 3.1 nM for human and mouse MAGL enzyme, respectively.

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    Biological Activity

    MAGLi 432 is a highly selective, potent and reversible monoacylglycerol lipase (MAGL) inhibitor with IC50 of 4.2 and 3.1 nM for human and mouse MAGL enzyme, respectively.
    MAGLi 432 selectively blocks binding of TAMRA-FP to MAGL but not to the active sites of other serine hydrolases in competitive activity based protein profiling (ABPP) assays.
    MAGLi 432 inhibits MAGL activity and MAGLi 432 (0.01-10 uM) robustly enhances 2-AG levels in human NVU cells.
    MAGLi 432 (1 mg/kg) achieves target occupancy and target engagement in a mouse model of LPS-induced neuroinflammation.
    MAGLi 432 treatment after LPS challenge does not ameliorate lipopolysaccharide-induced blood-brain barrier permeability in vivo or reduce the production of pro-inflammatory cytokines in the brain.

    Physicochemical Properties

    M.Wt 463.800
    Formula C22H24BrClN2O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (2-bromo-3-methoxyphenyl)((7R,9aR)-7-(4-chlorophenyl)octahydro-2H-pyrido[1,2-a]pyrazin-2-yl)methanone

    References

    1. Alicia Kemble, et al. bioRxiv 2022.05.04.490688.

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