Catalog No.: 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.
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.
