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Gefapixant citrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gefapixant citrate图片
CAS NO:2310299-91-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
MK-7264 citrate
AF-219 citrate
产品介绍
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。
生物活性

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& Target

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

体外研究
(In Vitro)

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].

体内研究
(In Vivo)

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].

Clinical Trial
分子量

545.52

Formula

C20H27N5O11S

CAS 号

2310299-91-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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