Overview
Alternative Name µ-theraphotoxin-Tp1a, µ-TRTX-Tp1a, Protoxin III, ProTx III
Lyophilized Powder yes
Origin Synthetic peptide
MW: 3802 Da
Purity: >98% (HPLC)
Effective concentration 1-250 nM
Sequence DCLKFGWKCNPRNDKCCSGLKCGSNHNWCKLHI-NH2
Modifications Disulfide bonds between Cys2-Cys17, Cys9-Cys22, and Cys16-Cys29. Ile 33 – C-terminal amidation.
Structure
Molecular formula C162H246N52O43S6
Activity ProTx-III is a potent blocker of NaV1.7 voltage-gated Na+ channels1.
References-Activity
- Cardoso, F.C. et al. (2015) Mol. Pharmacol. 88, 291.
Accession number P0DL64
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility Any other aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to two weeks at 4°C or three months at -20°C.
Our bioassay
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).
Scientific background
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.
Target NaV1.7 channels
Peptide Content: 100%
Lyophilized Powder
For research purposes only, not for human use
Last Update: 01/07/2024
Specifications
Citations
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