Agitoxin 2

Product Name:Agitoxin 2

CAS No:168147-41-9

Purity:95%

Molar Mass:4090.87

Chemical Formula:C169H278N54O48S8

Storage:Store at -20 degrees Celsius

Sequence:GVPINVSCTGSPQCIKPCKDAGMRFGKCMNRKCHCTPK

Target:K+ channel inhibitor

Application:

Agitoxin 2 is a peptide toxin derived from the venom of the scorpion Leiurus quinquestriatus. It functions as a potent inhibitor of voltage-gated potassium channels, specifically targeting the Kv1.3 channel. Kv1.3 channels are important in the regulation of immune cell activation, particularly in T cells. Because of its selective inhibition of Kv1.3, Agitoxin 2 is valuable in research related to autoimmune diseases, immunology, and ion channel pharmacology. It can help explore therapeutic approaches to modulating immune responses, particularly in conditions where Kv1.3 channels play a significant role, such as multiple sclerosis and rheumatoid arthritis.

Current Research:

Agitoxin-2 is a peptide toxin isolated from the venom of the scorpion Leiurus quinquestriatus hebraeus. Composed of 38 amino acids, this compact peptide is stabilized by three disulfide bridges, characteristic of scorpion toxins targeting ion channels. Agitoxin-2 is a potent and selective inhibitor of voltage-gated potassium channels (Kv), specifically Kv1.1 and Kv1.3, with high binding affinity and efficacy.
Mechanism of Action
Agitoxin-2 binds to the extracellular vestibules of Kv1.1 and Kv1.3 channels, occluding the pore and preventing potassium ion conduction. This blockage occurs through non-covalent interactions, effectively inhibiting the channels?? physiological function. By altering potassium ion flux, Agitoxin-2 modulates neuronal excitability and other cellular processes dependent on Kv channel activity.
The inhibition constants (K_d) for Agitoxin-2 are in the low nanomolar range, reflecting its high potency. Its selectivity for Kv1.1 and Kv1.3 channels over other Kv channel subtypes makes it a valuable research tool for studying the specific roles of these channels in physiological and pathological conditions.
Research Applications
Agitoxin-2 is widely utilized in neurophysiological and pharmacological studies to investigate:
The roles of Kv1.1 and Kv1.3 in neuronal signaling, immune function, and cardiac activity.
The mechanisms underlying diseases such as autoimmune disorders and channelopathies.
The development of therapeutic agents targeting Kv channels for conditions like multiple sclerosis and other immune-mediated diseases.
Conclusion
Agitoxin-2 provides a powerful means to explore Kv1.1 and Kv1.3 channel function, offering significant utility in neuroscience and ion channel research. Its high specificity and potency continue to inform therapeutic strategies targeting potassium channels.

Reference:

Sumino, A., Sumikama, T., Uchihashi, T., & Oiki, S. (2019). High-speed AFM reveals accelerated binding of agitoxin-2 to a K+ channel by induced fit. Science Advances, 5(7), eaax0495.