protx ii

Selective NaV1.7 channel blocker. Shifts activation gating positively and decreases current magnitude. Displays 100-fold selectivity over other sodium channel subtypes.

ProTx-II TFA是选择性作用于Nav1.7钠通道的阻滞剂，具有0.3 nM的IC50值，选择性比其他钠通道亚型高出至少100倍。该化合物抑制钠离子通道，通过减少通道电导及使激活电压向更正的电位移动，从而阻断痛觉感受器中动作电位的传导。

Potent Nav1.7 blocker (IC50 = 2.5 nM). Also inhibits Nav1.1, Nav1.2, Nav1.3 and Nav1.6 in the nanomolar range. Exhibits no effects on Cav channels or nAChR at 5 μM. Demonstrates analgesic activity in vivo; antagonizes effects of scorpion-venom toxin OD1 a

ProTx-III是一种从秘鲁绿绒狼蛛毒液中分离得到的蜘蛛毒肽，它是一个选择性且有效的Nav1.7电压门控钠离子通道抑制剂，其IC50值为2.1 nM。ProTx-III特征为含有典型的抑制剂胱氨酸结基序(ICK)，并可逆转疼痛反应，适用于慢性疼痛、癫痫和心律失常等疾病的研究。