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Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. It enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy [1].

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,900 | 8-10 weeks | 8-10 weeks | |
| 50 mg | $2,480 | 8-10 weeks | 8-10 weeks | |
| 100 mg | $3,400 | 8-10 weeks | 8-10 weeks |
| Description | Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. It enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy [1]. |
| In vitro | Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM) that selectively inhibits extrasynaptic α5-GABAARs in mouse CA1 pyramidal neurons[1]. |
| In vivo | Afizagabar (1 and 3 mg/kg; i.p.) significantly reduces the increase in total errors induced by Scopolamine[1]. |
| Molecular Weight | 365.38 |
| Formula | C19H12FN3O2S |
| Cas No. | 1398496-82-6 |
| Smiles | CC1=NN=C(c2cc3c(F)cccc3s2)c2cc3oc(=O)[nH]c3cc2C1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 6.25 mg/mL (17.11 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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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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