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BAY-1797 is an antagonist of the purinergic P2X4 receptor (IC50 = 0.211 µM for the human receptor).1 It is selective for P2X4 over P2X1, P2X3, and P2X7 receptors (IC50s = >50, 8.3, and 10.6 µM, respectively, for the human receptors), as well as a panel of G protein-coupled receptors (GPCRs), ion channels, kinases, and transporters at 10 µM. BAY-1797 (50 mg/kg) decreases intraplantar prostaglandin E2 (PGE2; Item No. 14010) levels and reduces non-evoked pain-related behavior in the dynamic weight bearing test in a mouse model of inflammatory pain induced by complete Freund’s adjuvant (CFA).
WARNING This product is not for human or veterinary use.
1. Discovery and characterization of the potent and selective P2X4 inhibitor N-