Gefapixant citrate 是一个口服有效的P2X3受体 (P2X3R) 拮抗剂，其对人同源重组 hP2X3 和 hP2X2/3 的IC50值分别是 ~30 nM 和 100-250 nM。Gefapixant citrate 可用于慢性咳嗽与膝骨关节炎的研究。

Gefapixant citrate is an orally active and potent purinergic P2X3 receptor ( P2X3R ) antagonist, with IC 50 values 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].

Gefapixant citrate displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC 50 values >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].

2310299-91-1

C20H27N5O11S

545.52

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years