| Name | E2730 |
| Description | E2730 is an orally active, selective, and non-competitive GABA transporter 1 (GAT1) inhibitor with antiepileptic activity, used in neurological disease research. |
| 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] |
| 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. |
| Keywords | GABAReceptor | GABA Receptor |
| Inhibitors Related | Valproic acid sodium salt | p-Hydroxybenzaldehyde | Urethane | Baicalin | Penicillin G sodium salt | Valproic Acid | Halothane | Chlorothymol | Piperazine citrate | (-)-α-Pinene | Dihydromyricetin | Methionine |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library |
United States
