7,8-Dihydroxyflavone

Catalog No.S8319 Batch:S831901

Technical Data

Formula	C₁₅H₁₀O₄
Molecular Weight	254.24	CAS No.	38183-03-8
Solubility (25°C)*	In vitro	DMSO	50 mg/mL (196.66 mM)
		Ethanol	1 mg/mL (3.93 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[3]}	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.
Animal Study:^{^[2]}	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.

Cell Assay:^{^[3]}

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.

Animal Study:^{^[2]}

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.

References

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

Polyphyllin VII induces CTC anoikis to inhibit lung cancer metastasis through EGFR pathway regulation [ Int J Biol Sci, 2023, 19(16):5204-5217]	PubMed: 37928267
Utility of 7,8-dihydroxyflavone in preventing astrocytic and synaptic deficits in the hippocampus elicited by PTSD [ Pharmacol Res, 2022, 176:106079]	PubMed: 35026406
Receptor-Independent Anti-Ferroptotic Activity of TrkB Modulators [ Int J Mol Sci, 2022, 23(24)16205]	PubMed: 36555849
Reduced BDNF expression in the auditory cortex contributed to neonatal pain-induced hearing impairment and dendritic pruning deficiency in mice [ Reg Anesth Pain Med, 2022, rapm-2022-103621]	PubMed: 36384877
Hippocampal neurogenesis interferes with extinction and reinstatement of methamphetamine-associated reward memory in mice [ Neuropharmacology, 2021, 196:108717]	PubMed: 34273388
Role of the BDNF/TrkB/CREB signaling pathway in the cytotoxicity of bisphenol S in SK-N-SH cells [ J Biochem Mol Toxicol, 2021, e22775]	PubMed: 33749030
Optimized integration of fluoxetine and 7, 8-dihydroxyflavone as an efficient therapy for reversing depressive-like behavior in mice during the perimenopausal period. [ Prog Neuropsychopharmacol Biol Psychiatry, 2020, 13;101:109939]	PubMed: 32243998
Nephronectin Expression is Inhibited by Inorganic Phosphate in Osteoblasts [ Calcif Tissue Int, 2019, 104(2):201-206]	PubMed: 30341591

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.