[CAS NO. 104104-50-9] Gabazine
PRODUCTS SPECIFICATIONS [104104-50-9]
DESCRIPTION [104104-50-9]
Overview
| MDL | MFCD09055424 |
|---|---|
| Molecular Weight | 368.23 |
| Molecular Formula | C15H18BrN3O3 |
| SMILES | O=C(O)CCCN1C(C=CC(C2=CC=C(OC)C=C2)=N1)=N.[H]Br |
2 Publications Citing Use of MCE
Summary
Gabazine is a selective and competitive antagonist of GABA A receptor , with an IC 50 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 IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 271.57 mM ; Need ultrasonic)
DMSO : ≥ 75 mg/mL ( 203.68 mM )
* "≥" means soluble, but saturation unknown.
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 |
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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
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2.
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3.
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
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4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution
Synonyms