Product Name:Cy5-ProTx-II
Purity:95%
Molar Mass:4450
Chemical Formula:C168H250N46O41S8
Storage:Store at -20 degrees Celsius
Sequence:Tyr-Cys2-Gln-Lys-Trp-Met-Trp-Thr-Cys9-Asp-Ser-Glu-Arg-Lys-Cys15-Cys16-Glu-Gly-Met-Val-Cys21-Arg-Leu-Trp-Cys25-Lys-Lys-Lys-Leu-Trp-OH
Target:NaV1.7 channels
Application:Cy5-ProTx-II is a fluorescently labeled variant of ProTx-II, a peptide toxin originally derived from the venom of the Thrixopelma pruriens tarantula. ProTx-II is a potent and selective inhibitor of voltage-gated sodium channels, particularly Nav1.7, which plays a critical role in pain signaling. By attaching the fluorescent dye Cy5 to ProTx-II, this modified peptide allows researchers to visualize and track the binding of the toxin to sodium channels in real-time, aiding in the study of sodium channel function, drug interactions, and mechanisms of pain. Cy5-ProTx-II is especially useful in fluorescence imaging and screening assays aimed at developing novel analgesics targeting Nav1.7 channels.
Current Research:
Cy5-ProTx-II is a fluorescently labeled derivative of ProTx-II, a peptide toxin originally isolated from the venom of the Peruvian green velvet tarantula (Thrixopelma pruriens). ProTx-II is renowned for its potent inhibition of voltage-gated sodium channels, particularly the Naᵥ1.7 subtype, which plays a crucial role in pain signaling pathways. The conjugation of the Cy5 fluorophore to ProTx-II enables real-time visualization and tracking of the peptide's interaction with sodium channels in various biological systems.
Structural and Functional Characteristics
ProTx-II is a 30-amino-acid peptide that adopts an inhibitor cystine knot (ICK) motif, contributing to its stability and affinity for sodium channels. The addition of the Cy5 fluorophore does not significantly alter the peptide's binding affinity or inhibitory potency. Cy5-ProTx-II retains high specificity for Naᵥ1.7 channels, with an IC₅₀ value of approximately 0.3 nM, and exhibits at least 100-fold selectivity over other sodium channel subtypes.
Applications in Research
The fluorescent properties of Cy5-ProTx-II make it an invaluable tool in neurophysiological and pharmacological research:
Visualization of Channel Distribution: Cy5-ProTx-II facilitates the mapping of Naᵥ1.7 channel distribution in tissues and cells, enhancing the understanding of channel localization and density.
Live-Cell Imaging: The Cy5 label allows for real-time observation of toxin-channel interactions in living cells, providing insights into the dynamics of channel function and regulation.
Drug Development: Cy5-ProTx-II serves as a probe in high-throughput screening assays aimed at identifying novel modulators of Naᵥ1.7 channels, which are potential therapeutic targets for pain management.
Handling and Storage
Cy5-ProTx-II is typically supplied as a lyophilized powder. For optimal stability, it should be stored at -20°C, protected from light and moisture. Upon reconstitution, aliquots should be prepared to avoid repeated freeze-thaw cycles, which can degrade the peptide.
Conclusion
Cy5-ProTx-II combines the potent inhibitory properties of ProTx-II with the fluorescent capabilities of the Cy5 dye, offering researchers a powerful tool to study Naᵥ1.7 sodium channels. Its application enhances the visualization and understanding of sodium channel physiology, contributing to advancements in neurobiology and the development of pain therapeutics.
Reference:
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