A potent blocker of Neuronal TTX-Sensitive Voltage-Gated Na+ Channel that preferentially inhibits neuronal voltage-gated sodium channel subtype hNav1.7 (SCN9A) (IC50 = 26 nM), rNav1.2 (SCN2A) (IC50 = 150 nM), and rNav1.3 (SCN3A) (IC50 = 338 nM), compared with muscle subtypes rNav1.4 (SCN4A) and hNav1.5 (SCN5A) (IC50 > 10 µM). Huwentoxin IV inhibits the activation of sodium channels by trapping the voltage sensor of domain II of the site 4 in the inward, closed configuration.
CAT No: R0984
CAS No:526224-73-7
Synonyms/Alias:526224-73-7;Huwentoxin-IV;Huwentoxin IV (Selenocosmia huwena venom);Huwentoxin IV;Huwentoxin IV TFA;BWA22473;AKOS024458310;DA-54140;PD079747;
Huwentoxin-IV (HWTX-IV), similarly to JZTX-34, inhibited neuronal TTX-sensitive voltage-gated sodium channels with an IC50 value of 30 nM in adult rat dorsal root ganglion neurons (DRG neurons), but have no significant effect on TTX-resistant voltage-gated sodium channels. Recently studies demonstrated that ProTx-II and HWTX-IV binding determinants on domain-II may overlap, with domain II playing a much more crucial role for HWTX-IV. The date also proved that the inhibition of sodium currents could be reversible by strong depolarization due to the dissociation of HWTX-IV.
Native Pyroglutamation of Huwentoxin-IV: A Post-Translational Modification that Increases the Trapping Ability to the Sodium Channel
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