nav1.7-in-3

Nav1.7-IN-3 is a selective and orally bioavailable inhibitor of voltage-gated sodium channel Nav1.7(IC50 of 8 nM).

4,9-Anhydrotetrodotoxin (4,9-anhydro-TTX) is a derivative of TTX that selectively blocks inward sodium current through Nav1.6 voltage-activated sodium channels (IC50 = 7.8 nM in Xenopus oocytes). [1][2][3] It demonstrates IC50 values of 1.3, 0.34, 0.99, 78.5, 1.3, and >30 µM for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.7, and Nav1.8, respectively.[1]

PF-06456384 trihydrochloride是一种高效和选择性 NaV1.7 抑制剂（IC50 =0.01 nM），通过蛋白质配体结合而不是抑制相关的钠通道发挥作用，专为静脉输注设计且可用于疼痛研究。

Potent rat Nav1.7, human Nav1.4 and rat Nav1.6 channel activator (EC50 values are 7, 10 and 47 nM, respectively). Exhibits minimal activation at mammalian Nav1.2, Nav1.3 and Nav1.5 (EC50 values >3 μM). Inhibits fast inactivation on all channels. Increases