Cyclotraxin B

Product Name:Cyclotraxin B

CAS No:1203586-72-4

Purity:95%

Molar Mass:1200.37

Chemical Formula:C48H73N13O17S3

Storage:Store at -20 degrees Celsius

Sequence:CNPMGYTKEGC

Target:TrkB

Application:

Cyclotraxin B is a small, cyclic peptide that acts as a selective and potent inhibitor of the TrkB (tropomyosin receptor kinase B) receptor, which is the main receptor for brain-derived neurotrophic factor (BDNF). BDNF and TrkB signaling are critical for neuronal survival, differentiation, and synaptic plasticity. By inhibiting TrkB, Cyclotraxin B is useful in research exploring the role of BDNF-TrkB signaling in neurodegenerative diseases, mood disorders, and synaptic plasticity. Its selective inhibition of TrkB makes Cyclotraxin B a valuable tool in studies related to neuroprotection, cognitive function, and therapeutic strategies for conditions such as depression, Alzheimer's disease, and neuroinflammation.

Current Research:

Cyclotraxin B is a cyclic peptide that functions as a highly potent and selective non-competitive antagonist of the tropomyosin receptor kinase B (TrkB), the primary receptor for brain-derived neurotrophic factor (BDNF). It inhibits BDNF-induced TrkB activity with an IC₅₀ of approximately 0.30 nM.

Structural Characteristics

Cyclotraxin B is composed of 10 amino acids, forming a cyclic structure stabilized by a disulfide bridge between cysteine residues at positions 1 and 11. This conformation contributes to its high stability and specificity in binding to TrkB receptors.

Mechanism of Action

As a non-competitive antagonist, Cyclotraxin B allosterically alters the conformation of TrkB receptors without interfering with BDNF binding. This modulation prevents receptor activation, thereby inhibiting downstream signaling pathways involved in synaptic plasticity, neuronal differentiation, and neuroprotection.

Pharmacological Significance

Cyclotraxin B has demonstrated the ability to cross the blood-brain barrier, making it a valuable tool for in vivo studies. In animal models, it has exhibited anxiolytic-like behavioral effects and has been shown to prevent BDNF-induced cold allodynia, indicating potential therapeutic applications in anxiety disorders and pain management.

Research Applications

Due to its high potency and selectivity, Cyclotraxin B is utilized in research to:

Investigate the role of TrkB signaling in neurological and psychiatric disorders.
Explore the mechanisms underlying synaptic plasticity and neuronal survival.
Develop potential therapeutic strategies targeting TrkB-related pathways.
Conclusion

Cyclotraxin B serves as a potent and selective tool for modulating TrkB activity, offering significant utility in both basic neuroscience research and the development of novel therapeutic approaches for conditions associated with dysregulated BDNF/TrkB signaling.

Reference:

Cazorla, M., Jouvenceau, A., Rose, C., Guilloux, J. P., Pilon, C., Dranovsky, A., & Prémont, J. (2010). Cyclotraxin-B, the first highly potent and selective TrkB inhibitor, has anxiolytic properties in mice. PloS one, 5(3), e9777.