E2730

Modify Date: 2024-09-23 19:25:36

E2730 Structure
E2730 structure
Common Name E2730
CAS Number 1520073-91-9 Molecular Weight 284.23
Density N/A Boiling Point N/A
Molecular Formula C9H8F4N2O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name E2730

 E2730 Biological Activity

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].
Related Catalog
Target

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

References

[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..  

 Chemical & Physical Properties

Molecular Formula C9H8F4N2O2S
Molecular Weight 284.23