MAGLi 432 | MAGL inhibitor | Probechem Biochemicals

Chemical Structure : MAGLi 432

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MAGLi 432 (MAGLi432)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	463.800
分子式	C22H24BrClN2O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

1. Alicia Kemble, et al. bioRxiv 2022.05.04.490688.

MAGLi 432 (MAGLi432)

生物&药学活性

物理化学性质&存储条件

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MAGLi 432 (MAGLi432)

生物&药学活性

物理化学性质&存储条件

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