nav1.3 channel

Nav1.3 Channel Inhibitor 1 (Compound 15b) is a state-dependent inhibitor of the voltage-gated sodium channel Na v 1.3, with an IC50 value of 20 nM. It has the ability to cross the blood-brain barrier, making it applicable for research into nervous system disorders [1].

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.

Scorpion toxin Tf2, a β-scorpion toxin first identified in the venom of the Brazilian scorpion Tityus fasciolatus, acts as an activator of the neuronal voltage-gated sodium (Nav) subtype Nav1.3, associated with epilepsy and nociception. It increases hNav1.3 activation voltage, prompting channel opening at resting membrane potentials [1].

GrTx1, a peptide toxin derived from Grammostola rosea spider venom, selectively inhibits sodium channels Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6, and Nav1.7, with IC50 values of 0.63 µM, 0.23 µM, 0.77 µM, 1.29 µM, 0.63 µM, and 0.37 µM, respectively [2]. This compound has applications in neurological disease research [1].

GTx1-15, an inhibitor cystine knot (ICK) peptide, antagonizes the voltage-dependent calcium channel Cav3.1, as well as voltage-dependent sodium channels Nav1.3 and Nav1.7 [1].

Ceratotoxin-2 (CcoTx2) is a voltage-gated sodium channel inhibitor with half maximal inhibitory concentrations (IC50) of 8 nM for Na v 1.2/β 1 and 88 nM for Na v 1.3/β 1 [1].

PF-05661014, a demethylated analogue of PF-06526290, selectively inhibits Nav1.3 and Nav1.7 currents by stabilizing the inactivated state through interaction with the D4 VSD. This compound is utilized in research focused on sodium channel modulation.

3'-Methoxydaidzein is a dual isoflavone and Sodium Channel inhibitor. 3'-Methoxydaidzein inhibited NaV1.7, NaV1.8 and NaV1.3 with IC50 of 181 nM, 397 nM and 505 nM, respectively. 3'-Methoxydaidzein was specific for collagen-induced platelet aggregation with IC50 values of 12.3 and 61.5µM, respectively. 3'-Methoxydaidzein acts as an analgesic by inhibiting voltage-gated sodium channels. 3'-Methoxydaidzein showed antioxidant activity and antiplatelet aggregation activity.

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

Potent and reversible Kv3.4 potassium channel blocker (IC50 = 47 nM); also attenuates inactivation of sodium currents by acting on Nav1.7 and Nav1.3 channels. Enhances TTX-sensitive sodium currents in rat small dorsal root ganglion neurons. Neuroprotective.