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PF 05089771 tosylate 是口服有效的、选择性的Nav1.7丙烯酰胺抑制剂。PF 05089771 tosylate 具有用于疼痛和糖尿病神经性疾病的研究。
PF 05089771 tosylate 是口服有效的、选择性的Nav1.7丙烯酰胺抑制剂。PF 05089771 tosylate 具有用于疼痛和糖尿病神经性疾病的研究。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 560 | 现货 | |
5 mg | ¥ 1,070 | 现货 | |
10 mg | ¥ 1,530 | 现货 | |
25 mg | ¥ 3,650 | 现货 |
产品描述 | PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50: 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50: 0.11-25 μM), L-type calcium, and KvLQT and hERG potassium channels (IC50: ≥10 μM), as well as human and cynomolgus monkey TRPV1 receptors (IC50: 10/20 μM). PF-05089771 is also 1, 000-fold selective for half-inactivated over resting Nav1.7 channels, and mutation of the domain IV voltage-sensor domain (VSD4) reduces PF-05089771 potency by approximately 100-fold. |
靶点活性 | Nav1.7 5N11S:11 nM , Nav1.7 5A11L:16 nM |
分子量 | 672.56 |
分子式 | C18H12Cl2FN5O3S2.C7H8O3S |
CAS No. | 1430806-04-4 |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | DMSO: 50 mg/mL |
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