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E2730 is an orally active, selective, and non-competitive GABA transporter 1 (GAT1) inhibitor with antiepileptic activity, used in neurological disease research.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $293 | In Stock | In Stock | |
| 5 mg | $722 | In Stock | In Stock | |
| 10 mg | $987 | In Stock | In Stock | |
| 25 mg | $1,520 | In Stock | In Stock | |
| 50 mg | $1,980 | In Stock | In Stock |
| Description | E2730 is an orally active, selective, and non-competitive GABA transporter 1 (GAT1) inhibitor with antiepileptic activity, used in neurological disease research. |
| Targets&IC50 | GAT-1 (human):1.1 μM, BGT1 (human):890 μM |
| In vitro | The 50% inhibition concentration (IC50) of E2730 was 1.1 μM for hGAT1, >1000 μM for hGAT2, >1000 μM for hGAT3, and 890 μM for hBGT-1. E2730 (0.0128-1000 μM) inhibited GAT1 in a non-competitive manner, and its inhibition was positively correlated with GABA levels in vitro. E2730 also increases extracellular GABA concentration under overactivation conditions. [1] |
| In vivo | E2730 (20-400mg/kg orally) showed antiepileptic effects in corneal ignition, 6 Hz-44 mA psychomotor seizures, amygdala ignition, Fragile X syndrome, and Dravet syndrome models. The 50% effective dose (ED50) of E2730 was 7.9 mg/kg in cornea-ignited mice and the 50% toxic dose (TD50) was 350 mg/kg in accelerated rotation tests. The E2730 has a protection index (i.e. the ratio of TD50 to ED50) of 44.3. [1] |
| Synonyms | E 2730 |
| Molecular Weight | 284.23 |
| Formula | C9H8F4N2O2S |
| Cas No. | 1520073-91-9 |
| Smiles | N(S(N)(=O)=O)[C@H]1C=2C(CC1(F)F)=CC(F)=CC2F |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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