1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor

6,2'-Dihydroxyflavone 

Cat. No.: HY-N6628 Purity: 99.10%
Handling Instructions

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

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

6,2'-Dihydroxyflavone Chemical Structure

6,2'-Dihydroxyflavone Chemical Structure

CAS No. : 92439-20-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
50 mg USD 60 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

GABAA receptor[1]

In Vitro

6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor. 6,2'-Dihydroxyflavone inhibits [3H]-flunitrazepam binding to the 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 (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].

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].

Solvent & Solubility
In Vitro: 

DMSO : 155 mg/mL (609.66 mM; Need ultrasonic and warming)

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
*Please refer to the solubility information to select the appropriate solvent.
References
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
Molecular Weight

254.24

Formula

C₁₅H₁₀O₄

CAS No.

92439-20-8

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
6,2'-Dihydroxyflavone
Cat. No.:
HY-N6628
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6,2'-Dihydroxyflavone

Cat. No.: HY-N6628