2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Flumazenil

Flumazenil  (Synonyms: Ro 15-1788)

Cat. No.: HY-B0009 Purity: 99.94%
COA Handling Instructions

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Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

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

Flumazenil Chemical Structure

Flumazenil Chemical Structure

CAS No. : 78755-81-4

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10 mM * 1 mL in DMSO
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Customer Review

Based on 3 publication(s) in Google Scholar

Flumazenil Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

In Vivo

Flumazenil interacts at the central benzodiazepine receptor to antagonize or reverse the behavioral, neurologic, and electrophysiologic effects of benzodiazepine agonists and inverse agonists. Flumazenil is of some benefit in hepatic encephalopathy, but until well-designed clinical trials are conducted, hepatic encephalopathy must be considered an investigational indication for flumazenil. Flumazenil has been shown to reverse sedation caused by intoxication with benzodiazepines alone or benzodiazepines in combination with other agents, but it should not be used when cyclic antidepressant intoxication is suspected[1]. Flumazenil (1 mg/kg) induces a strong anxiolytic effect in BALB/c mice tested in the elevated plus maze and light/dark test[2]. Flumazenil (10 mg/kg) effectively prevents the reduction produced by allopregnanolone in rats[3]. Flumazenil (5-20 mg/kg) antagonizes the anticonvulsant and adverse effects of diazepam but not GYKI 52466 in mice. Flumazenil slightly reduces the anticonvulsant activity of NBQX in the MES model but not in the PTZ test[4]. Flumazenil (3.0 mg/kg) blocks the changes withdrawal from chronic ethanol treatment, which leads to a decrease in open arm time and percent open arm entries[5].

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

303.29

Formula

C15H14FN3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C2CN(C(C3=CC(F)=CC=C3N2C=N1)=O)C)OCC
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 : 20 mg/mL (65.94 mM; ultrasonic and warming and heat to 60°C; 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 3.2972 mL 16.4859 mL 32.9717 mL
5 mM 0.6594 mL 3.2972 mL 6.5943 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 mg/mL (6.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (6.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.97%

COA (253 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[2]

Flumazenil is administered intraperitoneally in a volume of 10 mL/kg body weight 20 min before experimental testing. Two polyvinylchloride boxes (20×20×14 cm) covered with Plexiglas are connected by an opaque plastic tunnel (5×7×10 cm). One of these boxes is darkened. A light from a 100-W desk lamp 40 cm above the other box provided the only room illumination. This light level (300 lux) is chosen in order to avoid strain differences to be detected on time in the lit box (a measure of anxiety behaviour) in control animals. Indeed, in previous experiments, the BALB/c mice differ from C57BL/6 only in the high light condition. The subjects are individually tested in 5-min sessions between 1400 and 1700 hours. Mice are placed in the lit box to start the test session. The time spent in the lit box and the number of transitions from the dark box to the lit one are recorded after the first entry in the tunnel.

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

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2972 mL 16.4859 mL 32.9717 mL 82.4294 mL
5 mM 0.6594 mL 3.2972 mL 6.5943 mL 16.4859 mL
10 mM 0.3297 mL 1.6486 mL 3.2972 mL 8.2429 mL
15 mM 0.2198 mL 1.0991 mL 2.1981 mL 5.4953 mL
20 mM 0.1649 mL 0.8243 mL 1.6486 mL 4.1215 mL
25 mM 0.1319 mL 0.6594 mL 1.3189 mL 3.2972 mL
30 mM 0.1099 mL 0.5495 mL 1.0991 mL 2.7476 mL
40 mM 0.0824 mL 0.4121 mL 0.8243 mL 2.0607 mL
50 mM 0.0659 mL 0.3297 mL 0.6594 mL 1.6486 mL
60 mM 0.0550 mL 0.2748 mL 0.5495 mL 1.3738 mL
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Flumazenil Related Classifications

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:

Flumazenil78755-81-4Ro 15-1788GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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