nav1.7 in 2

Nav1.7-IN-2 is avoltage-gated sodium channels (Nav) inhibitor in particular Nav 1.7(IC50 of 80 nM).

ProTx-II TFA is a potent and highly selective Nav1.7 sodium channel blocker, exhibiting an IC50 of 0.3 nM and demonstrating at least 100-fold selectivity over other sodium channel subtypes. It decreases channel conductance, shifts activation towards more positive potentials, and inhibits action potential propagation in nociceptors [1] [2].

Ancistrotecine B (Compound 2), a Nav1.7 channel inhibitor (IC50: 0.73 μM), has been shown to alleviate inflammatory pain in mice [1].

Huwentoxin-IV TFA is a potent, selective blocker of sodium channels, specifically inhibiting neuronal Nav1.7, Nav1.2, Nav1.3, and Nav1.4 with IC50 values of 26, 150, 338, and 400 nM, respectively. It preferentially targets the peripheral nerve subtype Nav1.7 by interacting with neurotoxin receptor site 4, demonstrating analgesic effects in animal models of inflammatory and neuropathic pain [1] [2].

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].

LTGO-33 is a species-specific inhibitor of the voltage-gated sodium channel NaV1.8, inhibiting NaV1.8, NaV1.1-NaV1.7, and NaV1.9.LTGO-33 inhibits wild-type and multiple NaV1.8 variants associated with human pain disorders and can be used for the study of pain.hBChE-IN-2 is a low affinity Nurr1 agonist.

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]