E2730

• Description :

  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].

• CAS Number :

  [1520073-91-9]

• UNSPSC :

  12352005

• Target :

  GABA Receptor

• Type :

  Reference compound

• Related Pathways :

  Membrane Transporter/Ion Channel; Neuronal Signaling

• Applications :

  Neuroscience-Neuromodulation

• Field of Research :

  Neurological Disease

• Assay Protocol :

  https://www.medchemexpress.com/e2730.html

• Solubility :

  10 mM in DMSO

• Smiles :

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

• Molecular Formula :

  C9H8F4N2O2S

• Molecular Weight :

  284.23

• References & Citations :

  [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..

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2