E2730

CAT: 0804-HY-155238-01Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-155238-01Size:1 mg
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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].
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

Alternative Products

CatalogName
MBS5821061E2730

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