MilliporeSigma™ Calbiochem™ P2X Antagonist III

Description

• A phenylthio-nicotinamide that acts as a high affinity P2X 7 antagonist (pKi = 8.7 and 7.9, respectively, against 30nM A-804598 for rat and human P2X 7 binding) and potently inhibits P2X 7 -dependent cellular Ca 2+ mobilization (pIC 50 = 8.3, 7.5, and 7.2, respectively, using 1321N1 expressing human, mouse, or rat P2X 7 ; drug added 0.5 h prior to 3 min 0.25mm BzATP stimulation), while exhibiting much reduced or little potency toward a panel of 50 ion channels, transporters, and receptors
• Although not suitable for oral dosing due to high hepatic extraction ratios, effective delivery and brain P2X 7 occupancy can be achieved via s.c
• dosing in rats (30mg/kg) in vivo .