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

Gabazine (Synonyms: SR95531)

Cat. No.: HY-103533 Purity: >98.0%
Handling Instructions

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

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

Gabazine Chemical Structure

Gabazine Chemical Structure

CAS No. : 104104-50-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 330 In-stock
Estimated Time of Arrival: December 31
100 mg USD 590 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 75 mg/mL (203.68 mM)

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

368.23

Formula

C₁₅H₁₈BrN₃O₃

CAS No.

104104-50-9

SMILES

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

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:
Gabazine
Cat. No.:
HY-103533
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Gabazine

Cat. No.: HY-103533