Gefapixant citrate is an orally active and potent purinergicP2X3 receptor(P2X3R) antagonist, withIC₅₀values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis^[1][2][3].

IC50: ~30 nM (recombinant hP2X3 homotrimers), 100-250 nM (hP2X2/3 heterotrimeric receptors)^[1].

Gefapixant citrate displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC₅₀values >10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5 and hP2X7 channels)^[1].

Gefapixant citrate (7d bid, orally) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses in a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate)^[2].

545.52

C₂₀H₂₇N₅O₁₁S

2310299-91-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.