AR-C118925

AR-C118925 is a potent, selective, and non-nucleotide orthosteric antagonist of the **P2Y2 receptor (P2Y2R)**, a G protein-coupled receptor activated by extracellular nucleotides such as ATP and UTP. Originally developed as a pharmacological tool compound, it has been extensively utilized in preclinical research to investigate the role of P2Y2 signaling in various pathologies, including inflammatory diseases, cancer, renal disorders, and fibrosis. AR-C118925 blocks the canonical Gαq protein signaling pathway and other downstream effectors associated with P2Y2R activation. While it is a highly valuable lead compound for target validation, its therapeutic development has been hindered by poor pharmacokinetic properties, including high polarity and low oral bioavailability. Recent research efforts have focused on structure-based optimization of the AR-C118925 scaffold to develop more drug-like derivatives with improved metabolic stability and oral bioavailability.

Other names

AR-C