Home Protein Tyrosine Kinase Trk receptor agonist 7,8-Dihydroxyflavone For research use only.

7,8-Dihydroxyflavone

Synonyms: 7,8-DHF

7,8-Dihydroxyflavone (7,8-DHF) acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF).

7,8-Dihydroxyflavone Chemical Structure

7,8-Dihydroxyflavone Chemical Structure

CAS: 38183-03-8

Selleck's 7,8-Dihydroxyflavone has been cited by 8 publications

Purity & Quality Control

Batch: S831901 DMSO] 50 mg/mL] false] Ethanol] 1 mg/mL] false] Water] Insoluble] false Purity: 99.9%
99.9

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Biological Activity

Description 7,8-Dihydroxyflavone (7,8-DHF) acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF).
Targets
TrkB receptor [1]
(Cell-free assay)
320 nM(Kd)
In vitro
In vitro 7,8-DHF is one of the positive compounds that specifically activate TrkB, but not TrkA or TrkC, at a concentration of 250 nM. In addition to cortical and hippocampal neurons, 7,8-DHF also protects other cell types including the RGC (retinal ganglion cells) and PC12 cells from excitotoxic and oxidative stress-induced apoptosis and cell death. Thus, it has neuroprotective properties[1].
Cell Research Cell lines Rat pheochromocytoma (PC12) cells
Concentrations 1-25 μM
Incubation Time 1 h
Method

PC12 cells are seeded in 96-well plates at 104/well. After pretreatment with 7,8-DHF (1-25 μM) for 1 h, the cells are exposed to 6-OHDA (100 μM) for subsequent 24 h. The PI3k inhibitor LY294002 or MEK inhibitor PD98059 is added 30 min before 7,8-DHF treatment. At the end of the experiment, PC12 cells are incubated with 20 μl of MTT solution (5 mg/ml in PBS) for 4 h at 37 ◦C. The dark blue formazan product due to the reduction of MTT is dissolved in 150 μl of DMSO, and the absorbance at 570 nm is recorded with a microplate reader. The viability is expressed as the percentage of the untreated control cells.
In Vivo
In vivo 7,8-Dihydroxyflavone is a bioavailable chemical that can pass through the BBB to provoke TrkB and its downstream PI3K/Akt and MAPK activation in mouse brain upon intraperitoneal or oral administration. 7,8-DHF promotes the survival and reduces apoptosis in cortical neurons of traumatic brain injury as administration of 7,8-DHF at 3 h post-injury reduces brain tissue damage via the PI3K/Akt pathway. Its treatment does not induce any apparent toxicity in mice and is not toxic to the mice during the chronic treatment. 7,8-DHF displays robust therapeutic efficacy toward Alzheimer's disease and inhibits obesity through activating muscular TrkB[1].
Animal Research Animal Models Male Wistar rats; male APPswe/PS1dE9 transgenic mice
Dosages 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg and 3 mg/kg(Rats); 0.1 mg/kg(mice)
Administration i.p.

Chemical lnformation & Solubility

Molecular Weight 254.24 Formula

C15H10O4
CAS No. 38183-03-8 SDF Download 7,8-Dihydroxyflavone SDF
Smiles C1=CC=C(C=C1)C2=CC(=O)C3=C(O2)C(=C(C=C3)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (196.66 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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