Gefapixant citrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 IC50 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.

Gefapixant citrate displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC50 values >10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5 and hP2X7 channels).

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).

——

Others

Other Targets

Others

——

——

2310299-91-1

545.52

C20H27N5O11S

>98% (HPLC)

——

OC(=O)CC(O)(CC(O)=O)C(O)=O.COc1cc(C(C)C)c(Oc2cnc(N)nc2N)cc1S(N)(=O)=O

——

(-20℃)

With Ice Pack

≥ 2 years