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.
Synonyms:N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003
Molecular Formula:C₂₆H₃₀N₆O₃
Primary Target:P2X7
Primary Target IC50:18nM
Solubility:Warm DMSO
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.