6,2'-Dihydroxyflavone

Name: 6,2'-Dihydroxyflavone
Brand: MedChemExpress
SKU: HY-N6628
Rating: 4.5 (1 reviews)

Cat. No.: HY-N6628 Purity: 99.54%: FAQs
Data Sheet SDS COA Handling Instructions

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6,2'-Dihydroxyflavone is a novel antagonist of GABA_A receptor.

For research use only. We do not sell to patients.

6,2'-Dihydroxyflavone Chemical Structure

CAS No. : 92439-20-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

6,2'-Dihydroxyflavone is a novel antagonist of GABA_A receptor.

IC₅₀ & Target

GABA_A receptor^[1]

In Vitro

6,2'-Dihydroxyflavone is a novel antagonist of GABA_A receptor. 6,2'-Dihydroxyflavone inhibits [³H]-flunitrazepam binding to the rat cerebral cortex membranes with a K_i 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 (n=5), compare to a decrease to 65.9±3.0% by 1 μM FG-7142 (n=5). 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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

6,2'-Dihydroxyflavone-treated mice exhibit significant differences from control mice with respect to the percentage of open arms entries [F_(4,73)=8.01, P<0.0001] and the percentage of time spent in open arms [F_(4,73)=5.19, P<0.002], but not the number of entries to closed arms [F_(4,73)= 0.79,P=0.54]. The post-hoc NewmaneKeuls’ tests confirm that 6,2'-Dihydroxyflavone significantly decreases the percentage of open arm entries and time spent in open arms at the doses of 8 and 16 mg/kg. 6,2'-Dihydroxyflavone treatment similarly increases step-through latency [F_(4,75)=4.71, P<0.002], suggesting enhanced cognitive performance^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

254.24

Formula

C₁₅H₁₀O₄

CAS No.

92439-20-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C=C(C2=CC=CC=C2O)OC3=CC=C(O)C=C13

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (393.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

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: 99.54%

Select Batch:

Data Sheet (277 KB) SDS (581 KB)

COA (249 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Wang F, et al. 6,2'-Dihydroxyflavone, a subtype-selective partial inverse agonist of GABAA receptor benzodiazepine site. Neuropharmacology. 2007 Sep;53(4):574-82. [Content Brief]

Cell Assay ^[1]	Membranes from HEK 293T cell are used in this study. Briefly, aliquots of membranes are incubated with 1 nM [³H]-flunitrazepam or 8 nM [³H]-Ro15-4513 at 4°C for 90 min in the presence or absence of 6,2'-Dihydroxyflavone. After incubation, the mixtures are filtered onto Whatman GF/B filters with a Brandel 24-well harvester. Each filter is incubated for at least 1 h with 4 mL scintillation cocktail before measurement of radioactivity in a Beckman-Coulter LS 6500 scintillation counter. For saturation analysis, the membranes are incubated with increasing concentrations of [³H]-flunitrazepam or [³H]-Ro15-4513. Binding affinity is determined by nonlinear regression analysis^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Male ICR mice are randomized into six groups (n=12 to 16/group), and receive 0.4 mg/kg scopolamine (i.p.) 45 min prior to training, followed with vehicle (dd water, pH 9.0, p.o.), 2, 4, 8 or 16 mg/kg 6,2'-Dihydroxyflavone (p.o.), or 30 mg/kg FG-7142 (i.p.) 30 min prior to training. On the training trials, each mouse is placed into the lighted chamber of a two-compartment box, and the door leading to the dark chamber is opened 10 s later. Once the mouse enters the dark compartment, the door is closed and an inescapable electric foot-shock (0.4 mA, 1 s) is delivered from the grid floor. The mouse is removed from the apparatus 10 s later. The step-through latency is recorded, with the cut-off step-through latency set at 300 s^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Wang F, et al. 6,2'-Dihydroxyflavone, a subtype-selective partial inverse agonist of GABAA receptor benzodiazepine site. Neuropharmacology. 2007 Sep;53(4):574-82. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.9333 mL	19.6665 mL	39.3329 mL	98.3323 mL
	5 mM	0.7867 mL	3.9333 mL	7.8666 mL	19.6665 mL
	10 mM	0.3933 mL	1.9666 mL	3.9333 mL	9.8332 mL
	15 mM	0.2622 mL	1.3111 mL	2.6222 mL	6.5555 mL
	20 mM	0.1967 mL	0.9833 mL	1.9666 mL	4.9166 mL
	25 mM	0.1573 mL	0.7867 mL	1.5733 mL	3.9333 mL
	30 mM	0.1311 mL	0.6555 mL	1.3111 mL	3.2777 mL
	40 mM	0.0983 mL	0.4917 mL	0.9833 mL	2.4583 mL
	50 mM	0.0787 mL	0.3933 mL	0.7867 mL	1.9666 mL
	60 mM	0.0656 mL	0.3278 mL	0.6555 mL	1.6389 mL
	80 mM	0.0492 mL	0.2458 mL	0.4917 mL	1.2292 mL
	100 mM	0.0393 mL	0.1967 mL	0.3933 mL	0.9833 mL