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| Product | Description | |
|---|---|---|
| A 740003 | A 740003. Group: Biochemicals. Grades: Purified. CAS No. 861393-28-4. Pack Sizes: 10mg, 50mg. US Biological Life Sciences. |  Worldwide |
| 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. Synonyms: 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. Grades: >98 %. CAS No. 861393-28-4. Molecular formula: C26H30N6O3. Mole weight: 474.55. |  |
| A740003 (N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2, 2-dimethylpropyl) -2- (3, 4-dimethoxyphenyl) acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003) | 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. Group: Biochemicals. Grades: Highly Purified. CAS No. 861393-28-4. Pack Sizes: 5mg. Molecular Formula: C??H??N?O?, Primary Target: P2X7. US Biological Life Sciences. | Worldwide |
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