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Chemical Structure : MAGLi 432
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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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.
| M.Wt | 463.800 | |
| Formula | C22H24BrClN2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Alicia Kemble, et al. bioRxiv, 2022.
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