Gabazine (Synonyms: SR95531)

Name: Gabazine
Brand: MedChemExpress
SKU: HY-103533
Rating: 5.0 (9 reviews)

Cat. No.: HY-103533 Pureza: 98.72%: Ficha de datos
COA

SDS
Instrucciones de manejo
FAQs
Technical Support

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

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 104104-50-9

Tamaño	Stock	Cantidad

Muestra gratis (0.1 - 0.2 mg)	Solicite ahora
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

or Consulta para venta a granel

* Seleccione Cantidad antes de agregar artículos.

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

Revisión del cliente

Based on 9 publication(s) in Google Scholar

Other Forms of Gabazine:

Gabazine free base Obtener un presupuesto
Gabazine (Standard) Obtener un presupuesto

9 Publications Citing Use of MCE Gabazine

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: Gabazine purchased from MedChemExpress. Usage Cited in: Nature. 2025 Oct;646(8087):1243-1253. [Abstract]; A small fraction of the currents remained in two cells, after d-AP5 exposure, presented a shape consistent with GABAA receptor-mediated currents and could be inhibited with the GABAA receptor blocker Gabazine (Gbz) (12.5 μM).

: Gabazine purchased from MedChemExpress. Usage Cited in: Elife. 2024 May 29.; The effects of ICV injection of different doses of Gabazine (2 or 4 μg/mL; 2000 nL) on the recovery time of midazolam. Compared with the vehicle, ICV injection of Gabazine could reduce the recovery time.

: Gabazine purchased from MedChemExpress. Usage Cited in: Elife. 2024 May 29.; The peak ΔF/F in the Before RORR and RORR-Recovery stages with or without intracerebroventricular injection of Gabazine (4 μg/mL). Gabazine could increase the ΔF/F peak of calcium signaling in LCNE neurons.

: Gabazine purchased from MedChemExpress. Usage Cited in: Elife. 2024 May 29.; The effects of intra-LC injection of Gabazine (4 μg/mL)and intra-VLPO injection of prazosin on the recovery time of midazolam. Microinjection of Gabazine into the LC could reduce the recovery time.

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

Gabazine is a selective and competitive antagonist of GABA_A 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 GABA_A 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.

Peso molecular

368.23

Fòrmula

C₁₅H₁₈BrN₃O₃

No. CAS

104104-50-9

Appearance

Solid

Color

White to off-white

SMILES

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, sealed storage, away from moisture

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

Solvente y solubilidad

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
10 mM	0.2716 mL	1.3578 mL	2.7157 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.

Calculadora de molaridad
Calculadora de dilución

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 (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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.79 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.

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)

Dosing volume
(per animal)

μL

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).

Pureza y Documentación

Purity: 98.72%

Select Batch:

Ficha de datos (272 KB) SDS (393 KB)

COA (246 KB) HNMR (289 KB) RP-HPLC (248 KB) MS (68 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Ueno S, et al. Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptor. J Neurosci. 1997 Jan 15;17(2):625-34. [Content Brief]

Complete Stock Solution Preparation Table

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.

Gabazine Related Classifications

Neurological 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:

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

Productos vistos recientemente:

Nombre del producto

Requested Quantity *

Nombre del solicitante *

Saludo

Direcciòn del E-mail *

Número de teléfono *

Department

Nombre de la Organizaciòn *

City

Provincia

Country or Region *

Observaciones

Nombre del producto

Lot #

Nombre del solicitante *

Direcciòn del E-mail *

Número de teléfono

Department *

Nombre de la Organizaciòn *

Country or Region *

Observaciones

Name
E-mail *

	Sorry, but the email address you supplied was invalid.

Gabazine (Synonyms: SR95531)

Revisión del cliente

Other Forms of Gabazine:

Gabazine Related Antibodies

9 Publications Citing Use of MCE Gabazine

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Gabazine Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Gabazine Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report