- Cardoso, F.C. et al. (2015) Mol. Pharmacol. 88, 291.
- Alomone Labs ProTx-III inhibits NaV1.7 currents heterologously expressed in Xenopus oocytes.A.Time course of ProTx-III (#STP-150) blocking action on NaV1.7 currents. Maximum current amplitudes were plotted as a function of time. Membrane potential was held at -100 mV and cells were stimulated by a 100 ms voltage step to -10 mV. 250 nM ProTx-III were perfused as indicated by the bar (green) during 4 min application. B. Superimposed examples of NaV1.7 channel current in the absence (control) and presence (green) of 250 nM ProTx-III (taken from the experiment in A).
ProTx-III (µ-TRTX-Tp1a) originally isolated from the venom of the peruvian green-velvet tarantula Thrixopelma pruries, is a potent blocker of voltage-gated sodium (NaV) channels, with highest affinity towards NaV1.7 with an IC50 of 11.5 nM, and demonstrates analgesic properties in in vivo models1.
NaV channels are responsible for initiating action potentials in electrically excitable cells. They play an important role in the human pain signalling pathway and are important therapeutic targets for treatment of chronic pain. Mutations in NaV channels are also associated with a range of complex pathologic conditions such as epilepsy, myotonic conditions and cardiac arrhythmias1,2.
ProTx-III (#STP-150) is a highly pure, synthetic, and biologically active peptide toxin.