A cell permeable flavone based compound with neurotrophic and neuroprotective properties. Mimicks the action of Brain Derived Neurotrophic Factor (BDNF) and acts as a TrkB receptor agonist. Due to its lipophilic nature, it can cross the blood-brain barrier. Binds to the extra cellular domain of TrkB with high affinity and promotes its dimerization and autophosphorylation. Potentiates TrkB, but not TrkA, signaling in mouse brain slices. Its neurotropic effects are abolished in the presence of K252a. Suppresses apoptosis in human and rodent neurons and in stably transfected TrkB murine cell line T48 (EC50 = 35 nM). Selectively reduces the basal GABAergic transmission due to its suppressive effect on presynaptic GABA release. However, it does not affect glutamatergic transmission.
Biochem/physiol Actions
Cell permeable: yes
Primary Target TrkB
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Ren, Q., et al. 2013. Pharm. Biochem. Behav.106, 124. Marongiu, D., et al. 2013. Eur. J. Pharmacol.709, 64. Jang, S., et al. 2010. PNAS107, 2687.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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