Purity ~98% (HPLC). A highly potent, selective, competitive antagonist of P2X7 purinegic receptor (IC50 = 18nM and 40nM, respectively as measured by Bz-ATP-stimulated Ca2+ flux). Does not affect other P2 receptors even at 10uM concentrations. Blocks agonist-evoked IL-1b release (IC50 = 156nM) and pore formation (IC50 = 92nM) in differentiated human THP-1 cells. Also shown to reduce carrageenan and Freund's adjuvant -induced thermal hyperalgesia (ED50 = 38-54mg/kg, i.p) and neuropathic pain induced by chronic constriction injury (CIC) of the sciatic nerve. Primary Target: P2X7 Primary Target IC50: 18nM Solubility: Warm DMSO