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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phospholipase-BRI-50460
BRI-50460

Chemical Structure : BRI-50460

CAS No.:

BRI-50460 (BRI 50460, BRI50460)

货号: PC-26014Not For Human Use, Lab Use Only.

BRI-50460 is a potent, selective and brain-penetrant cytosolic calcium-dependent phospholipase A2 (cPLA2) inhibitor with IC50 of 0.88 nM for cellular arachidonic acid (AA) release and 4.1 nM for downstream PGE2 production.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BRI-50460 is a potent, selective and brain-penetrant cytosolic calcium-dependent phospholipase A2 (cPLA2) inhibitor with IC50 of 0.88 nM for cellular arachidonic acid (AA) release and 4.1 nM for downstream PGE2 production.
BRI-50460 demonstrates high selectivity, exhibiting negligible inhibition of iPLA2 in in vitro fluorescence assays at 50 uM.
BRI-50460 mitigates the effects of amyloid beta 42 oligomers on cPLA2 activation, tau hyperphosphorylation, and synaptic loss in astrocytes and neurons derived from human induced pluripotent stem cells.

物理化学性质&存储条件

分子量 394.45
分子式 C21H18N2O4S
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

N-(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)-3-phenoxybenzenesulfonamide

参考文献

1. Sadybekov AV, et al. NPJ Drug Discov. 2026;3(1):2. doi: 10.1038/s44386-025-00035-0.

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