| 货号 | 21256-1mg |
| 描述 | A-740003 is a competitive antagonist of the ATP-gated ionotropic P2X7 receptor (IC50s = 40 and 18 nM for human and rat receptors, respectively).1 It shows weak or no activity at other P2 receptors and other receptors and ion channels. A-740003 blocks agonist-induced IL-1β release and pore formation in differentiated THP-1 cells (IC50s = 156 and 92 nM, respectively).1 It is effective in vivo when administered intraperitoneally, reducing pain in several animal models.1 A-740003 is used in cell and animal studies to elucidate P2X7 roles and signaling pathways.2,3,4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Honore, P.,Donnelly-Roberts, D.,Namovic, M.T., et al. A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J. Pharmacol. Exp. Ther. 319(3), 1376-1385 (2006). 2.Donnelly-Roberts, D.L. and Jarvis, M.F. Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states. British Journal of Pharmacology 151(5), 571-579 (2007). 3.Gicquel, T.,Robert, S.,Loyer, P., et al. IL-1β production is dependent on the activation of purinergic receptors and NLRP3 pathway in human macrophages. FASEB J. 29(10), 4162-4173 (2015). 4.Grol, M.W.,Brooks, P.J.,Pereverzev, A., et al. P2X7 nucleotide receptor signaling potentiates the Wnt/β-catenin pathway in cells of the osteoblast lineage. Purinergic Signal. 12(3), 509-520 (2016). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 474.6 |
| 分子式 | C26H30N6O3 |
| CAS号 | 861393-28-4 |
| 稳定性 | ≥ 2 years |
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