APETx2

Product Name:APETx2

Synonyms:Toxin APETx2, Pi-AITX-Ael2b, Pi-actitoxin-Ael2b

CAS No:713544-47-9

Purity:95%

Molar Mass:4561

Chemical Formula:C196H280N54O61S6

Storage:Store at -20 degrees Celsius

Sequence:GTACSCGNSKGIYWFYRPSCPTDRGYTGSCRYFLGTCCTPAD.

Target:ASIC3 channels

Application:

APETx2 is a peptide toxin derived from the sea anemone Anthopleura elegantissima. It is a selective inhibitor of acid-sensing ion channels (ASIC3), which are involved in pain perception, especially in acidic conditions such as inflammation and ischemia. By blocking ASIC3, APETx2 has become a valuable tool in pain research, particularly for studying chronic and inflammation-related pain disorders. Researchers utilize APETx2 to explore the role of ASIC3 in pain pathways and to develop potential new treatments for pain management. Its specificity for ASIC3 makes it a promising candidate for investigating novel analgesic therapies targeting these ion channels.

Current Research:

APETx2 is a 42-amino-acid peptide toxin isolated from the sea anemone Anthopleura elegantissima. It functions as a selective and reversible inhibitor of acid-sensing ion channel 3 (ASIC3), a proton-gated sodium channel implicated in pain perception.

Structural Characteristics

APETx2 comprises 42 amino acids and is stabilized by three disulfide bridges, forming a compact structure. Its three-dimensional conformation includes a four-stranded β-sheet, characteristic of the disulfide-rich all-β structural family commonly found in animal venom peptides.

Mechanism of Action

APETx2 selectively inhibits ASIC3 by binding to the channel's extracellular domain, thereby preventing proton-induced activation. This inhibition is reversible, with an IC₅₀ of approximately 63 nM, indicating high potency.

Pharmacological Significance

By inhibiting ASIC3, APETx2 has demonstrated the ability to reverse acid-induced and inflammatory pain in animal models, highlighting its potential as a novel analgesic agent.

Research Applications

APETx2 serves as a valuable tool in neurophysiological research, particularly in studies exploring the role of ASIC3 in pain pathways and sensory neuron function. Its specificity and potency make it instrumental in elucidating the physiological and pathological roles of ASIC3.

Reference:

Chagot, B., Escoubas, P., Diochot, S., Bernard, C., Lazdunski, M., & Darbon, H. (2005). Solution structure of APETx2, a specific peptide inhibitor of ASIC3 proton‐gated channels. Protein science, 14(8), 2003-2010.