nav1.6

NaV1.2/1.6 channel blocker-1 is a potent inhibitor of NaV1.2 and NaV1.6 channels, exhibiting inhibitory effects on rNaV1.6 and hNaV1.2. This compound can be utilized in the study of generalized epilepsy and movement disorders.

GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype-selective Nav1.7 inhibitor [Ki: 0.79 nM, Kd: 0.38 nM for hNav1.7] for the treatment of chronic pain.

Nav1.1 activator 1 (compound 4) is an effective Nav1.1 agonist with blood-brain barrier permeability, exhibiting significant selectivity for Nav1.2, Nav1.5, and Nav1.6. It increases the decay time constant of Nav1.1 at 0.03 μM current and can be used for studying central nervous system disorders.

XPC-6444 is a isoform-selective, and CNS-penetrant inhibitor of NaV1.6 with IC50 of41 nM for hNaV1.6,with anticonvulsant activity.

SYM2206 is a low affinity non-competitive AMPA receptor antagonist with an IC50 value of 1.6 μM.SYM2206 exhibits anticancer activity by blocking Nav1.6-mediated sustained currents and decreasing the survival of pancreatic cancer cells.

XPC-7724 is a selective inhibitor of the Nav1.6 channel, with an IC50 value of 0.078 μM. It is useful in research related to neurological disorders.

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective positive modulator of Nav1.1 channels and also increases the activity of Nav1.2 and Nav1.5 channels while not affecting Nav1.4, Nav1.6, and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

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]

GDC-0310 is a selective, orally available Nav1.7 inhibitor with an IC50 of 0.6 nM for human Nav1.7, suitable for pain research.

AA43279 is a novel selective Nav1.1 activator, increasing the firing activity of parvalbumin-expressing, fast-spiking GABAergic interneurons and increasing the spontaneous inhibitory post-synaptic currents (sIPSCs) recorded from pyramidal neurons.

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.

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].

GsAF-I is a potent blocker of Na_v and hERG1 channels, exhibiting half-maximal inhibitory concentrations (IC50s) of 0.36 μM (Na_v 1.1), 0.6 μM (Na_v 1.2), 1.28 μM (Na_v 1.3), 0.33 μM (Na_v 1.4), 1.2 μM (Na_v 1.6), 0.04 μM (Na_v 1.7), and 4.8 μM (hERG1) [1].

XPC-5462 effectively inhibits NaV1.6 and NaV1.2 channels with IC50 values of 10.9 nM and 10.3 nM, respectively, and reduces epileptiform activity in an ex vivo brain slice seizure model [1].

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

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

Poneratoxin acetate is a neurotoxic peptide and modulator of NaV1.6/NaV1.7, lowering the activation threshold of voltage-gated sodium channels and causing pain.