925463-91-8

Selective blocker of NaV5 channels (IC50 = 348 nM); displays no effect on other isoforms, including NaV2, NaV4, NaV6 and NaV7. Thought to inhibit sodium channel activation by binding to the NaV5 S3-S4 linker of domain II. Selectively inhibits the activation of cardiac sodium channels, but has no effect on sodium channels in dorsal root ganglion neurons.

Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype[1][2].

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[1] Rong M, et, al. Molecular basis of the tarantula toxin jingzhaotoxin-III (β-TRTX-Cj1α) interacting with voltage sensors in sodium channel subtype Nav1.5. FASEB J. 2011 Sep; 25(9): 3177-85. DOI:10.1096/fj.10-178848
[2] Xiao Y, et, al. Jingzhaotoxin-III, a novel spider toxin inhibiting activation of voltage-gated sodium channel in rat cardiac myocytes. J Biol Chem. 2004 Jun 18; 279(25): 26220-6. DOI:10.1074/jbc.M401387200