2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. 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).

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E2730 Chemical Structure

E2730 Chemical Structure

CAS No. : 1520073-91-9

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E2730 Related Antibodies

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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].

IC50 & Target

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

284.23

Formula

C9H8F4N2O2S
CAS No.
SMILES

FC1=C2C(CC(F)(F)[C@H]2NS(N)(=O)=O)=CC(F)=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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E2730 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

E27301520073-91-9E 2730E-2730GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorGABA transportersGAT1anti-seizure medicationsuncompetitive inhibitionInhibitorinhibitorinhibit

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