Phrixotoxin 3

Product Name:Phrixotoxin 3

CAS No:880886-00-0

Purity:95%

Molar Mass:4059.72

Chemical Formula:C176H269N51O48S6

Storage:Store at -20 degrees Celsius

Sequence:DCLGFLWKCNPSNDKCCRPNLVCSRKDKWCKYQI

Target:voltage-gated sodium channels

Application:

Phrixotoxin 3 is a peptide toxin that specifically inhibits voltage-gated sodium channels (Nav), particularly Nav1.2. These sodium channels are crucial for the initiation and propagation of action potentials in neurons and muscle cells. By blocking Nav channels, Phrixotoxin 3 is a valuable tool for studying neuronal excitability and the role of sodium channels in various physiological processes. It is used in research to explore potential therapeutic applications for conditions such as epilepsy, chronic pain, and other neurological disorders where sodium channel dysfunction plays a significant role.

Current Research:

Phrixotoxin-3 is a peptide toxin derived from the venom of the tarantula Phrixotrichus auratus. It functions as a potent inhibitor of voltage-gated sodium channels (Nav), particularly targeting the Nav1.2 subtype.
Structural Characteristics
Phrixotoxin-3 consists of 35 amino acids and is stabilized by three disulfide bridges, forming a compact structure typical of spider toxins that modulate ion channel activity.
Mechanism of Action
Phrixotoxin-3 modulates voltage-gated sodium channels by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current. This dual action prevents the channels from opening in response to moderate depolarization, resulting in a reduced firing rate of neurons.
Selectivity and Potency
Phrixotoxin-3 exhibits varying inhibitory potency across different Nav channel subtypes, with reported half-maximal inhibitory concentration (IC??) values of:
Nav1.2: 0.6 nM
Nav1.3: 42 nM
Nav1.4: 72 nM
Nav1.1: 288 nM
Nav1.5: 610 nM
These values indicate a high affinity for Nav1.2 channels, making Phrixotoxin-3 a valuable tool for studying the physiological roles of this specific sodium channel subtype.
Research Applications
Due to its specificity and potency, Phrixotoxin-3 is utilized in neurophysiological research to:
Investigate the function of Nav1.2 channels in neuronal excitability.
Explore the pathophysiological mechanisms underlying neurological disorders associated with sodium channel dysfunction.
Develop potential therapeutic agents targeting specific sodium channel subtypes.
Conclusion
Phrixotoxin-3 serves as a potent and selective inhibitor of voltage-gated sodium channels, particularly Nav1.2, offering significant utility in both basic and applied neuroscience research.

Reference:

Bosmans, F., Rash, L., Zhu, S., Diochot, S., Lazdunski, M., Escoubas, P., & Tytgat, J. (2006). Four novel tarantula toxins as selective modulators of voltage-gated sodium channel subtypes. Molecular pharmacology, 69(2), 419-429.