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

Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.

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Gabazine Chemical Structure

Gabazine Chemical Structure

CAS No. : 104104-50-9

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Based on 6 publication(s) in Google Scholar

Other Forms of Gabazine:

Gabazine Related Antibodies

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  • Purity & Documentation

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Description

Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.

IC50 & Target

0.2 μM (GABA receptor)[1].
In Vitro

Both bicuculline and Gabazine (SR 95531) have been characterized as competitive inhibitors of GABA binding to the GABAA receptor. Gabazine is more potent than bicuculline at blocking currents elicited by GABA, with an IC50 for currents elicited by 3 μM GABA of ~0.2 μM and a Hill coefficient of 1.0. Gabazine reduces the currents elicited by 10 μM alphaxalone by ~30%, for responses of receptors containing wildtype β2 subunits. The concentration of Gabazine requires producing half the maximal block is ~0.2 μM. Gabazine also could only produce a partial block of currents gated by 300 μM pentobarbital. The maximal reduction, again, is ~30%, and the concentration of Gabazine required to produce half the maximal block is ~0.15 μM[1].

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

Gabazine Related Antibodies
Molecular Weight

368.23

Formula

C15H18BrN3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CCCN1C(C=CC(C2=CC=C(OC)C=C2)=N1)=N.[H]Br
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (271.57 mM; Need ultrasonic)

DMSO : ≥ 75 mg/mL (203.68 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 2.7157 mL 13.5785 mL 27.1569 mL
5 mM 0.5431 mL 2.7157 mL 5.4314 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (6.79 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.79 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 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 7.14 mg/mL (19.39 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.05%

COA (246 KB) HNMR (262 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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 / H2O 1 mM 2.7157 mL 13.5785 mL 27.1569 mL 67.8923 mL
5 mM 0.5431 mL 2.7157 mL 5.4314 mL 13.5785 mL
10 mM 0.2716 mL 1.3578 mL 2.7157 mL 6.7892 mL
15 mM 0.1810 mL 0.9052 mL 1.8105 mL 4.5262 mL
20 mM 0.1358 mL 0.6789 mL 1.3578 mL 3.3946 mL
25 mM 0.1086 mL 0.5431 mL 1.0863 mL 2.7157 mL
30 mM 0.0905 mL 0.4526 mL 0.9052 mL 2.2631 mL
40 mM 0.0679 mL 0.3395 mL 0.6789 mL 1.6973 mL
50 mM 0.0543 mL 0.2716 mL 0.5431 mL 1.3578 mL
60 mM 0.0453 mL 0.2263 mL 0.4526 mL 1.1315 mL
80 mM 0.0339 mL 0.1697 mL 0.3395 mL 0.8487 mL
100 mM 0.0272 mL 0.1358 mL 0.2716 mL 0.6789 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Gabazine 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:

Gabazine104104-50-9SR95531SR 95531SR-95531GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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