| Identification | Back Directory | [Name]
Methanone, (2-bromo-3-methoxyphenyl)[(7R,9aR)-7-(4-chlorophenyl)octahydro-2H-pyrido[1,2-a]pyrazin-2-yl]- | [CAS]
2361575-20-2 | [Synonyms]
Methanone, (2-bromo-3-methoxyphenyl)[(7R,9aR)-7-(4-chlorophenyl)octahydro-2H-pyrido[1,2-a]pyrazin-2-yl]- [(7R,9aR)-7-(4-chlorophenyl)-1,3,4,6,7,8,9,9a-octahydropyrido[1,2-a]pyrazin-2-yl]-(2-bromo-3-methoxyphenyl)methanone | [Molecular Formula]
C22H24BrClN2O2 | [MOL File]
2361575-20-2.mol | [Molecular Weight]
463.8 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
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[1]. | Animal Model: | Male CD-1 mice model of LPS-induced neuroinflammation[1] | | 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.
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| [References]
[1] Alicia Kemble, et al. A potent and selective inhibitor for the modulation of MAGL activity in the neurovasculature. bioRxiv 2022.05.04.490688. |
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