| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Human recombinant α1β2γ2L GABAA receptor; Human recombinant α1β2 GABAA receptor [1]
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|---|---|
| ln Vitro |
6-Mmethylflavone activates GABAA receptors α1β2η2L and α1β2. 6-Mmethylflavone improved, at doses ranging from 1 to 100 μM (P<0.0001), the typical response of recombinant α1β2η2L and α1β2 GABAA receptors to GABA. 6-Methylflavone (60 μM) decreases the average EC50 of α1β2η2L GABAA receptors by 33±5.4%[1] and moves the GABA dose-response curve to the left (n=4, F=16.38, P=0.0004).
6-Methylflavone acts as a flumazenil-independent positive modulator of gamma-aminobutyric acid (GABA) action at human recombinant GABAA receptors. In cells expressing α1β2γ2L GABAA receptors, it concentration-dependently enhanced GABA-induced inward currents: at 10 μM, the current amplitude was increased by 1.8-fold, and at 30 μM, it was increased by 2.5-fold compared to GABA alone [1] In cells expressing α1β2 GABAA receptors, 6-Methylflavone also concentration-dependently potentiated GABA-induced currents: 10 μM caused a 1.6-fold increase, and 30 μM caused a 2.2-fold increase. This potentiation was not blocked by flumazenil (a selective benzodiazepine site antagonist), indicating a distinct binding site from benzodiazepines [1] |
| Enzyme Assay |
Human embryonic kidney (HEK) 293 cells were transfected with plasmids encoding human α1β2γ2L or α1β2 GABAA receptor subunits and cultured until suitable for electrophysiological recording. Cells were voltage-clamped at a holding potential of -60 mV using the whole-cell patch-clamp technique. GABA was applied at a concentration that induced 10–20% of the maximum current response, and 6-Methylflavone was co-applied at serial concentrations (1, 10, 30 μM) to assess potentiation. To test flumazenil independence, flumazenil was pre-incubated with cells for 5 minutes before co-application with 6-Methylflavone and GABA. Current responses were recorded and analyzed to calculate the fold potentiation relative to GABA alone [1]
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| References | |
| Additional Infomation |
6-Methylflavonoids are a type of flavonoid compound. 6-Methylflavonoids are a flavonoid derivative with positive regulatory activity on GABAA receptors [1]. Its mechanism of action involves enhancing GABA-mediated chloride ion influx through GABAA receptors, thereby enhancing inhibitory neurotransmission. Unlike benzodiazepines, its regulatory effect is not antagonized by flumazenil, suggesting that it binds to a unique allosteric site on the GABAA receptor [1].
|
| Molecular Formula |
C16H12O2
|
|---|---|
| Molecular Weight |
236.2653
|
| Exact Mass |
236.084
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| CAS # |
29976-75-8
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| PubChem CID |
689013
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| Appearance |
White to light yellow solid powder
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| Density |
1.208g/cm3
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| Boiling Point |
395.5ºC at 760mmHg
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| Melting Point |
119-122 °C (dec.)(lit.)
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| Flash Point |
183.8ºC
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| Vapour Pressure |
1.83E-06mmHg at 25°C
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| Index of Refraction |
1.623
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| LogP |
3.768
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
|
| Heavy Atom Count |
18
|
| Complexity |
352
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NOQJBXPAMJLUSS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H12O2/c1-11-7-8-15-13(9-11)14(17)10-16(18-15)12-5-3-2-4-6-12/h2-10H,1H3
|
| Chemical Name |
6-methyl-2-phenylchromen-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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~211.62 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.58 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 (10.58 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 | 4.2324 mL | 21.1622 mL | 42.3245 mL | |
| 5 mM | 0.8465 mL | 4.2324 mL | 8.4649 mL | |
| 10 mM | 0.4232 mL | 2.1162 mL | 4.2324 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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