A bisalykylsulfonamide that acts as a positive, allosteric modulator against AMPA receptors (EC50 = 45nM and 63nM for GluA2i and GluA2o, respectively) in a HEK 293 calcium FLIPR assay. At 10uM, it robustly modulates receptor desensitization of both the flip (GluA2i) and flop (GluA2o) isoforms of GluA2 receptors in transfected HEK 293 cells with higher potency and efficacy than two other distinct AMPA modulators, cyclothiazide and CX614. Using a ligand bound crystal structure, it is shown to bind to the dimer interface of the extracellular ligand-binding domain of AMPA receptors, a region that partially overlaps with binding pockets for cyclothiazide and CX614.
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
