A cell-permeable thiazolidinedione that acts as a PPARg-selective agonist (Ki=160nM) and blocks Cdk-5-mediated Ser273 phosphorylation by stabilizing PPARg b-sheet structure, exhibiting no detectable activity towards PPARa, PPARd, or RXRa. Although a weaker PPAPg agonist than Thiazolidinediones (TZDs) family rosiglitazone (Max. fold of transactivation induction =8.57 and 24.8 with 10uM respective compound in U-937 reporter assays), GQ-16 can be safely administered at a higher dosage (20mg/kg/day; oral gavage) in mice to achieve similar in vivo efficacy as rosiglitazone (4mg/kg/day; o.g.) without adverse side effects commonly seen with TZDs.
Formula:C19H16BrNO3S
Molecular Weight:418.3
Solubility:DMSO (5mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. 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.
