6-Methoxyflavanone
Based on 1 Customer Validation
6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of GABAA receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABAA receptors, and is relatively inactive on the α1β2 GABAA receptor. 6-Methoxyflavanone showes inhibitory behavior towards the activation of bitter receptor hTAS2R39 and hTAS2R14, demonstrating a reversible and non-overcome antagonistic effect. 6-Methoxyflavanone has the effects of anti-anxiety, analgesia and relief of neuropathic pain.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 3034-04-6
- Formula: C16H14O3
- Molecular Weight:254.28
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 ADR | IC50 |
39 μM
Compound: 1
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Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay
Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay
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[PMID: 21354800] |
| MCF7 | IC50 |
46 μM
Compound: 1
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Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining
Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining
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[PMID: 21354800] |
| MDCK | IC50 |
19 μM
Compound: 1
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Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining
Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining
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[PMID: 21354800] |
| MDCK | IC50 |
64 μM
Compound: 1
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Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry
Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry
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[PMID: 21354800] |
6-Methoxyflavanone (0-1000 μM) inhibits hTAS2R39 and hTAS2R14 activated by Epicatechin gallate (ECG) (HY-N0002) with IC50 values of 479 μM and 447 μM when it is pre-treated and then added to the ECG in HEK293 cells[1].
6-Methoxyflavanone can significantly regulate α1β2γ2L and α2β2γ2L receptors in X. oocytes with EC50 of 43.7 and 52.2 μM, respectively, it is also a partial agonist of q1W328M GABA receptor with EC50 of 51.6 μM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC |
|---|---|---|---|---|---|---|
| Mice[1] | 30 mg/kg | i.p. | 46.23 min | 30 min | 2.73 μg/mL | 1.05 μg·h/mL |
6-Methoxyflavanone (10-300 mg/kg, i.p., single dose) attenuates mechanical allodynia and vulvodynia in the Streptozotocin (HY-13753)-induced diabetic neuropathic pain at 10 and 30 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Behavioral analysis, elevated plus-maze, staircase test and open-field test established in BALB/c mice (18-30 g) of both sex[1]
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Dosage:10, 30, 50 and 100 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Reduced the viral load in the spleen by more than 33 times.
Exerted an anxiolytic-like effect, increasing entries and time spent in the open arm and the central platform, as well as head-dipping frequency in the mouse elevated plus-maze assay at 10, 30 and 50 mg/kg.
Decreased rearing incidence without suppressing the number of steps ascended in the staircase test.
Had no effect on locomotor activity at lower doses, a decrease was observed at the highest dose (100 mg/kg).
Produced an anxiolytic-like increase in the time spent at the center of the open-field apparatus.
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Animal Model:Streptozotocin-induced diabetic neuropathic pain model established female Sprague-Dawley rats (150-200 g) and BALB/c mice (18-30 g)[2]
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Dosage:30, 50, 100, 150 and 300 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Demonstrated dose-dependent analgesic effect at hot plate test (acute phasic thermal nociception).
Significantly improved the pain symptoms caused by diabetes.
Observed no significant toxic reactions were at a dose of up to 300 mg/kg.
Chemical Information
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CAS No. 3034-04-6
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Appearance Solid
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Molecular Weight 254.28
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Formula C16H14O3
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Color Off-white to light yellow
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SMILES
O=C1CC(C2=CC=CC=C2)OC3=CC=C(OC)C=C13
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Synonyms
6-MeOF
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (393.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Akbar S, et al. Characterization of 6-methoxyflavanone as a novel anxiolytic agent: A behavioral and pharmacokinetic approach. Eur J Pharmacol. 2017 Apr 15;801:19-27. [Content Brief]
[2]. Akbar S, et al. 6-Methoxyflavanone attenuates mechanical allodynia and vulvodynia in the streptozotocin-induced diabetic neuropathic pain. Biomed Pharmacother. 2016 Dec;84:962-971. [Content Brief]
[3]. Roland WS, et al. 6-methoxyflavanones as bitter taste receptor blockers for hTAS2R39. PLoS One. 2014 Apr 10;9(4):e94451. [Content Brief]
[4]. Hall BJ, et al. Modulation of ionotropic GABA receptors by 6-methoxyflavanone and 6-methoxyflavone. Neurochem Res. 2014 Jun;39(6):1068-78. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.9327 mL | 19.6634 mL | 39.3267 mL | 98.3168 mL |
| 5 mM | 0.7865 mL | 3.9327 mL | 7.8653 mL | 19.6634 mL | |
| 10 mM | 0.3933 mL | 1.9663 mL | 3.9327 mL | 9.8317 mL | |
| 15 mM | 0.2622 mL | 1.3109 mL | 2.6218 mL | 6.5545 mL | |
| 20 mM | 0.1966 mL | 0.9832 mL | 1.9663 mL | 4.9158 mL | |
| 25 mM | 0.1573 mL | 0.7865 mL | 1.5731 mL | 3.9327 mL | |
| 30 mM | 0.1311 mL | 0.6554 mL | 1.3109 mL | 3.2772 mL | |
| 40 mM | 0.0983 mL | 0.4916 mL | 0.9832 mL | 2.4579 mL | |
| 50 mM | 0.0787 mL | 0.3933 mL | 0.7865 mL | 1.9663 mL | |
| 60 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.6386 mL | |
| 80 mM | 0.0492 mL | 0.2458 mL | 0.4916 mL | 1.2290 mL | |
| 100 mM | 0.0393 mL | 0.1966 mL | 0.3933 mL | 0.9832 mL |
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