E2730

SKU: orb1944269

Description

E2730 is a selective, non-competitive inhibitor of the GABA transporter 1 (GAT1) with oral bioavailability. It is used in research to study epilepsy and other neurological disorders, with applications in both in vitro binding assays and in vivo seizure models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1520073-91-9
• MW: 284.23
• Purity: 98.22% (May vary between batches)
• Formula: C₉H₈F₄N₂O₂S
• SMILES: N(S(N)(=O)=O)[C@H]1C=2C(CC1(F)F)=CC(F)=CC2F
• Target: GABA Receptor

Bioactivity

• Target IC50:
  GAT-1 (human):1.1 μM|BGT1 (human):890 μM
• In Vivo:
  E2730 (20-400mg/kg orally) showed antiepileptic effects in corneal ignition, 6 Hz-44 mA psychomotor seizures, amygdala ignition, Fragile X syndrome, and Dravet syndrome models. The 50% effective dose (ED50) of E2730 was 7.9 mg/kg in cornea-ignited mice and the 50% toxic dose (TD50) was 350 mg/kg in accelerated rotation tests. The E2730 has a protection index (i.e. the ratio of TD50 to ED50) of 44.3.
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• In Vitro:
  The 50% inhibition concentration (IC50) of E2730 was 1.1 μM for hGAT1, >1000 μM for hGAT2, >1000 μM for hGAT3, and 890 μM for hBGT-1. E2730 (0.0128-1000 μM) inhibited GAT1 in a non-competitive manner, and its inhibition was positively correlated with GABA levels in vitro. E2730 also increases extracellular GABA concentration under overactivation conditions.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GABAReceptor, GABA Receptor, E 2730

Compound Identifiers

PubChem CID

72694819