E2730 

E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg)^[1].

γ-aminobutyric acid (GABA) transporter 1 (GAT1)^[1]

284.23

C₉H₈F₄N₂O₂S

1520073-91-9

FC1=C2C(CC(F)(F)[C@H]2NS(N)(=O)=O)=CC(F)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Fukushima K, et al. Discovery of E2730, a novel selective uncompetitive GAT1 inhibitor, as a candidate for anti-seizure medication. Epilepsia Open. 2023 Sep;8(3):834-845..  [Content Brief]