产品
编 号：F751508
分子式：C22H24BrClN2O2
分子量：463.8
分子式：C22H24BrClN2O2
分子量：463.8
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CAS No: 2361575-20-2
产品详情
生物活性：
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. 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). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease.
体内研究：
MAGLi 432 (intraperitoneal injection, 1 mg/kg for 3 consecutive days) inhibits MAGL in the brain and reduces arachidonic acid and PGE2 levels in LPS-induced neuroinflammation, without reducing BBB permeability and inflammatory cytokine expression in the cortex.Animal Model:Male CD-1 mice model of LPS-induced neuroinflammation
Dosage:1 mg/kg for 3 consecutive days
Administration:Intraperitoneal injection
Result:Accumulated ~10-fold more 2-AG than vehicle controls, reducted LPS-induced PGE2.Increased LCN2 and TNF expression compared to the LPS treatment.
体外研究：
MAGLi 432 (10 μΜ, 25 min) displays selectivity and potency for MAGL over other serine hydrolases in mouse and human brain lysates.MAGLi 432 (1 μΜ, 6 h) inhibits MAGL activity and robustly enhances 2-AG levels in human NVU cells.
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. 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). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease.
体内研究：
MAGLi 432 (intraperitoneal injection, 1 mg/kg for 3 consecutive days) inhibits MAGL in the brain and reduces arachidonic acid and PGE2 levels in LPS-induced neuroinflammation, without reducing BBB permeability and inflammatory cytokine expression in the cortex.Animal Model:Male CD-1 mice model of LPS-induced neuroinflammation
Dosage:1 mg/kg for 3 consecutive days
Administration:Intraperitoneal injection
Result:Accumulated ~10-fold more 2-AG than vehicle controls, reducted LPS-induced PGE2.Increased LCN2 and TNF expression compared to the LPS treatment.
体外研究：
MAGLi 432 (10 μΜ, 25 min) displays selectivity and potency for MAGL over other serine hydrolases in mouse and human brain lysates.MAGLi 432 (1 μΜ, 6 h) inhibits MAGL activity and robustly enhances 2-AG levels in human NVU cells.
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