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A-740003 A-740003 is potent, selective and competitive P2X7 receptor antagonist. Its IC50 values are 18 and 40 nM for rat and human receptors respectively measured by agonist-stimulated changes in intracellular calcium concentrations. It displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. It reduces nociception in animal models of persistent neuropathic and inflammatory pain. It showed weak or no activity (IC(50) > 10 muM) at other P2 receptors and an array of other neurotransmitter and peptide receptors, ion channels, reuptake sites, and enzymes. It potently blocked agonist-evoked IL-1beta release (IC(50) = 156 nM) and pore formation (IC(50) = 92 nM) in differentiated human THP-1 cells. It produces significant antinociception in animal models of neuropathic and inflammatory pain in vivo. Uses: A-740003 produces significant antinociception in animal models of neuropathic and inflammatory pain in vivo. Group: Pharmaceutical. Alternative Names: A-740003; A 740003; A740003; N-[1-[[(Cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide;N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide. CAS No. 861393-28-4. Pack Sizes: 1mg;1g;10g. Product ID: 861393-28-4. Molecular formula: C26H30N6O3. Mole weight: 474.55. Custom synthesis is available. Send your inquiries for more information. BOC Sciences
London

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