6-Methoxyflavanone (Synonyms: 6-MeOF)

Cat. No.: HY-N8852 Purity: 98.95%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of GABA_A receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABA_A receptors, and is relatively inactive on the α1β2 GABA_A 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.

6-Methoxyflavanone Chemical Structure

CAS No. : 3034-04-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	Get quote
10 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A2780 ADR	IC₅₀	39 μM Compound: 1	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	[PMID: 21354800]
MCF7	IC₅₀	46 μM Compound: 1	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	[PMID: 21354800]
MDCK	IC₅₀	19 μM Compound: 1	Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining	[PMID: 21354800]
MDCK	IC₅₀	64 μM Compound: 1	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	[PMID: 21354800]

In Vitro

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.

Parmacokinetics^[1]

Species	Dose	Route	Indicator	value
Mice	30 mg/kg	i.p.	T_1/2	46.23 min
Mice	30 mg/kg	i.p.	T_max	30 min
Mice	30 mg/kg	i.p.	C_max	2.73 μg/mL
Mice	30 mg/kg	i.p.	AUC	1.05 μg·h/mL

In Vivo

6-methoxyflavanone (10-100 mg/kg, i.p., single dose) penetrates the blood brain barrier (BBB) generating in mice anxiolytic activity, most probably mediated via Flumazenil (HY-B0009)-insensitive pentylenetetrazole binding sites^[1].
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.

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]
Dosage:	10, 30, 50 and 100 mg/kg
Administration:	Intraperitoneal injection (i.p.), single dose
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.

Animal Model:	Streptozotocin-induced diabetic neuropathic pain model established female Sprague-Dawley rats (150-200 g) and BALB/c mice (18-30 g)^[2]
Dosage:	30, 50, 100, 150 and 300 mg/kg
Administration:	Intraperitoneal injection (i.p.), single dose
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.

Molecular Weight

254.28

Formula

C₁₆H₁₄O₃

CAS No.

3034-04-6

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1CC(C2=CC=CC=C2)OC3=CC=C(OC)C=C13

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.9327 mL	19.6634 mL	39.3267 mL
5 mM	0.7865 mL	3.9327 mL	7.8653 mL
10 mM	0.3933 mL	1.9663 mL	3.9327 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 98.95%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (247 KB) HNMR (240 KB) LCMS (98 KB)

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

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

6-Methoxyflavanone Related Classifications

Neurological Disease Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

6-Methoxyflavanone3034-04-66-MeOFGABA ReceptorTaste ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorFlavonoidanxietyGABAA receptorselevated plus-mazestaircase anxiety testInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

6-Methoxyflavanone (Synonyms: 6-MeOF)

6-Methoxyflavanone Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

6-Methoxyflavanone Related Antibodies

Molarity Calculator

Dilution Calculator