Size : 10mg
Synonyms:
| Description | GABAA receptor modulator-9 is a positive allosteric modulator of the GABAA receptor, specifically targeting the α1β2γ2 subtype and capable of crossing the blood-brain barrier. It exhibits excellent activity at α1β2γ2 (EC50: 0.9 μM in oocytes and 0.2 μM in CHO cells) and also shows activity at α1β2, α3β2γ2, and α1β3γ2 (with EC50 values of 1.3, 3.4, and 1.1 μM, respectively). GABAA receptor modulator-9 significantly inhibits seizure progression and reduces mortality in mice. It is applicable in studies of status epilepticus (SE). |
| In vitro | GABAA receptor modulator-9 (Compound (S)-9d) shows the greatest selectivity for the α1 subunit, likely without displaying selectivity for the β subunit, and the γ2 subunit does not affect its allosteric activity on GABAA receptors. |
| In vivo | The compound GABAA receptor modulator-9 ((S)-9d), when administered intraperitoneally at doses of 5-30 mg/kg (single dose), prevents 90% of mice from experiencing stage V seizures and significantly delays the onset of status epilepticus induced by Pilocarpine, as well as acute convulsions triggered by Pentylenetetrazol. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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