7,8-Dihydroxyflavone

For research use only.

Catalog No.S8319 Synonyms: 7,8-DHF

4 publications

7,8-Dihydroxyflavone Chemical Structure

CAS No. 38183-03-8

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).

Selleck's 7,8-Dihydroxyflavone has been cited by 4 publications

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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

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].

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].

Protocol

Cell Research:

[3]

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  • 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.


    (Only for Reference)
Animal Research:

[2]

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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 50 mg/mL (196.66 mM)
Ethanol 1 mg/mL (3.93 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 254.24
Formula

C15H10O4

CAS No. 38183-03-8
Storage powder
in solvent
Synonyms 7,8-DHF
Smiles C1=CC=C(C=C1)C2=CC(=O)C3=C(O2)C(=C(C=C3)O)O

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Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID