Prototoxin 2 ProTx-II

Article number:

5250048

Formula:

C168H250N46O41S6

Chemical description:

Sequence: [Cys2-Cys16, Cys9-Cys21, Cys15-Cys25 ]; H-Tyr-Cys-Gln-Lys-Trp-Met-Trp-Thr-Cys-Asp-Ser-Glu-Arg-Lys-Cys-Cys-Glu-Gly-Met-Val-Cys-Arg-Leu-Trp-Cys-Lys-Lys-Lys-Leu-Trp-OH

Molecular weight:

3833,00 g/mol

Inhibits voltage-gated calcium and sodium channels (site 4). Inhibits activation by shifting the voltage-dependence of channel activation to more positive potentials. Potently inhibits all sodium channel subtypes tested (Nav1.2/SCN2A, Nav1.5/SCN5A, Nav1.7/SCN9A, and Nav1.8/SCN10A). Is approximately 15-fold more potent on Nav1.7/SCN9A than on Nav1.5/SCN5A channels. Acts on Cav3.1/CACNA1G, and interacts more weakly with the related T-Type channel Cav3.2/CACNA1H but potently inhibits the L-type calcium channel Cav1.2/CACNA1C. Binds to phospholipids. ProTx-II, a selective inhibitor of Nav1.7 sodium channels, blocks action potential propagation in nociceptors.

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Prototoxin 2 ProTx-II

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