A selective, irreversible inhibitor of GABA transaminase with antiepileptic properties. Covalently binds to the active site of GABA tansaminase to inactivate it in a dose-dependent manner and increases extracellular GABA levels in the brain. Rapidly absorbed following oral administration and is shown to inhibit [3H]GABA uptake across the apical membrane of Caco-2 cell monolayers in a concentration-dependent manner (IC50 = 2.9mM).
Solubility:H2O
Primary Target:GABA Transaminase
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
