| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Targets |
6,2'-Dihydroxyflavone targets the GABAA receptor, which is the major inhibitory neurotransmitter receptor in the central nervous system. It acts as a novel antagonist of the GABAA receptor, inhibiting the binding of GABA to its receptor and thereby modulating inhibitory neurotransmission. The compound inhibits [3H]-flunitrazepam binding to rat cerebral cortex membranes with a Ki of 37.2 ± 4.5 nM.
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| ln Vitro |
6,2'-DiHydroxyflavone is a novel antagonist of GABAA receptors. With a Ki of 37.2±4.5 nM, 6,2'-Dihydroxyflavone prevents [3H]-flunitrazepam from binding to rat cerebral cortex membranes. The current generated by GABA EC50 concentration was lowered to 73.6±1.9% of control when co-administered 5 μM 6,2'-dihydroxyflavone (n=5), whereas that of 1 μM FG was reduced to 65.9±3.0% -7142 (n= 5). The maximal GABA current dropped and the EC50 of the GABA dosage response rose from 47.6 μM to 59.7 μM following the co-administration of 5 μM 6,2'-dihydroxyflavone [1].
In vitro, 6,2'-Dihydroxyflavone acts as a GABAA receptor antagonist. It inhibits [3H]-flunitrazepam binding to rat cerebral cortex membranes with a Ki of 37.2 ± 4.5 nM. The current elicited with the EC50 concentration of GABA is decreased to 73.6 ± 1.9% of control by co-application of 5 µM 6,2'-Dihydroxyflavone. The EC50 for GABA dose response increases from 47.6 to 59.7 µM upon co-application of 5 µM 6,2'-Dihydroxyflavone, and the maximal GABA-current is decreased. |
| ln Vivo |
The number of times entering the closed arm [F(4,73)= 0.79, P=0.54] is not as significant as the percentage of 6,2'-dihydroxyflavone-treated mice entering the open arm [F (4,73)=8.01, P<0.0001] or the percentage of time spent in the open arm [F (4,73)=5.19, P<0.002]. At dosages of 8 mg/kg and 16 mg/kg, 6,2'-dihydroxyflavone significantly decreased the percentage of open arm entry and time spent in the open arm, according to Newmane-Keuls post hoc testing. Step latency is similarly increased by 6,2'-dihydroxyflavone treatment [F(4,75)=4.71, P<0.002], suggesting improved cognitive function [1].
In vivo, 6,2'-Dihydroxyflavone-treated mice exhibit significant differences from control mice with respect to the percentage of open arm entries and the percentage of time spent in open arms in the elevated plus maze test. This suggests that the compound modulates anxiety-like behavior through its antagonistic action at GABAA receptors. The compound shows potential for neuroprotective applications based on its ability to modulate GABAergic neurotransmission. |
| Enzyme Assay |
In vitro receptor binding assays for 6,2'-Dihydroxyflavone involve measuring its affinity for the GABAA receptor using radioligand binding techniques. The compound inhibits [3H]-flunitrazepam binding to rat cerebral cortex membranes. Membranes are incubated with increasing concentrations of the compound and a fixed concentration of [3H]-flunitrazepam, and the Ki value is determined from competition binding curves. These cell-free assays provide quantitative data on the compound's receptor binding affinity.
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| Cell Assay |
In vitro cellular assays for 6,2'-Dihydroxyflavone are performed using cells expressing GABAA receptors, such as primary neurons or recombinant cell lines. The compound's antagonist activity is assessed by measuring GABA-induced currents using patch-clamp electrophysiology. Cells are treated with GABA in the presence and absence of the compound, and the reduction in GABA-induced current is quantified. These assays provide functional evidence of the compound's GABAA receptor antagonism.
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| Animal Protocol |
In vivo animal experiments for 6,2'-Dihydroxyflavone are conducted in mouse models to assess behavioral effects. A typical protocol involves administration of the compound to mice, followed by behavioral testing such as the elevated plus maze to evaluate anxiety-like behavior. The percentage of open arm entries and time spent in open arms are measured as indicators of anxiolytic or anxiogenic effects. These studies help characterize the in vivo pharmacological effects of GABAA receptor antagonism.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 6,2'-Dihydroxyflavone have not been systematically characterized. The compound has a molecular weight of 254.24 and molecular formula C15H10O4. It is a solid with solubility in DMSO ≥100 mg/mL. The compound should be stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years. Further PK studies are needed to determine its absorption and distribution profile.
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| Toxicity/Toxicokinetics |
Toxicological data for 6,2'-Dihydroxyflavone are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
6,2'-Dihydroxyflavone is a flavonoid compound with CAS number 92439-20-8, molecular formula C15H10O4, and molecular weight 254.24. It is also known as 6-hydroxy-2-(2-hydroxyphenyl)-4H-chromen-4-one. It functions as a novel GABAA receptor antagonist with a Ki of 37.2 ± 4.5 nM. The compound has demonstrated antioxidant, anti-inflammatory, and neuroprotective effects and is used in neuroscience research.
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| Molecular Formula |
C15H10O4
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| Molecular Weight |
254.2375
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| Exact Mass |
254.058
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| CAS # |
92439-20-8
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| PubChem CID |
688661
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.871
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
390
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YCGXYGWBHFKQHY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10O4/c16-9-5-6-14-11(7-9)13(18)8-15(19-14)10-3-1-2-4-12(10)17/h1-8,16-17H
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| Chemical Name |
6-hydroxy-2-(2-hydroxyphenyl)chromen-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~393.33 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9333 mL | 19.6665 mL | 39.3329 mL | |
| 5 mM | 0.7867 mL | 3.9333 mL | 7.8666 mL | |
| 10 mM | 0.3933 mL | 1.9666 mL | 3.9333 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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