Lu AF27139 | P2X7 antagonist | Probechem Biochemicals

Chemical Structure : Lu AF27139

CAS No.: 2097117-06-9

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Lu AF27139 (Lu AF 27139)

货号: PC-38015Not For Human Use, Lab Use Only.

Lu AF27139 is a potent, selective, CNS-penetrant P2X7 receptor antagonist, inhibits BzATP-induced currents in rat primary microglia with IC50 of 66 nM.

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5 mg	￥1980	In stock
10 mg	￥2980	In stock
25 mg	￥4880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Lu AF27139 is a potent, selective, CNS-penetrant P2X7 receptor antagonist, inhibits BzATP-induced currents in rat primary microglia with IC50 of 66 nM.
Lu AF27139 is highly selective and potent against rat, mouse, and human forms of the receptors.
Lu AF27139 concentration-dependently inhibits IL-1β release in rat ((C50=38 nM) and mouse (IC50=26 nM) primary cortical microglia primed with LPS and induced with 1 mM BzATP.
Lu AF27139 displays favorable PK profile with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability.
Lu AF27139 inhibits LPS- and BzATP-induced IL-1β release in in vivo mouse CNS microdialysis studies.

物理化学性质&存储条件

分子量	497.921
分子式	C21H19ClF3N5O2S
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	(S)-N-(2-(4-chlorophenyl)-2-morpholinoethyl)-2-(pyrimidin-2-yl)-4-(trifluoromethyl)thiazole-5-carboxamide

参考文献

1. Allen T Hopper, et al. J Med Chem. 2021 Apr 22;64(8):4891-4902.

Lu AF27139 (Lu AF 27139)

生物&药学活性

物理化学性质&存储条件

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Lu AF27139 (Lu AF 27139)

生物&药学活性

物理化学性质&存储条件

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