| 货号 | 5931/50 |
| 别名 | 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-ch |
| 供应商 | Tocris |
| 生物活性 | Potent and selective Nav1.7 channel blocker (IC50 = 8, 11 and 171 nM for mouse, human and rat Nav1.7, respectively). Exhibits selectivity for Nav1.7 over other Nav1 channels (IC50 values are 0.11, 0.16, 0.85, 10, 11 and 25 μM for Nav1.2, Nav1.6, Nav1.1, Nav1.4, Nav1.3 and Nav1.5, respectively). Also exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. Blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro. |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >98 % |
| 计算分子量 | 672.56 |
| 分子式 | C18H12Cl2FN5 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| 参考文献 | Alexandrouet al (2016) Subtype-selective small molecule inhibitors reveal a fundamental role for Nav1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release. PLoS One 11 e0152405. PMID: 27050761. Caoet al (2016) Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia. Sci.Transl.Med. 8 335ra56. PMID: 27099175. |