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A cell-permeable thiophene carboxymide derived compound that acts as a direct and selective antagonist of TrkB receptor. Binds to the high affinity site on the extracellular domain of TrkB in a dose-dependent manner (Kd = 10 nM) exhibiting much reduced binding to the low affinity site (Kd =12 µM) indicating that it does not compete with BDNF for the same binding site. Does not affect TrkA or TrkC receptors. Shown to permeate the blood-brain barrier, however, its antagonistic effects are not uniform throughout the brain. Does not affect the survivability of neurons. Reduces anxiety and depression related behavior in mice.
Cazorla, M., et al. 2011. J. Clin. Invest.121,1846.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
A cell-permeable thiophene carboxymide derived compound that acts as a direct and selective antagonist of TrkB receptor. Binds to the high affinity site on the extracellular domain of TrkB in a dose-dependent manner (Kd = 10 nM) exhibiting much reduced binding to the low affinity site (Kd =12 µM) indicating that it does not compete with BDNF for the same binding site. Does not affect TrkA or TrkC receptors. Shown to permeate the blood-brain barrier, however, its antagonistic effects are not uniform throughout the brain. Does not affect the survivability of neurons. Reduces anxiety and depression related behavior in mice.
Form
White solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
219766-25-3
Chemical formula
C₂₂H₂₁N₃O₃S
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (25 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Cazorla, M., et al. 2011. J. Clin. Invest.121,1846.
