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Gefapixant
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图片
CAS NO:1015787-98-0
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议

产品名称
RO 4926219
MK-7264
AF219
产品介绍
Gefapixant 是一个 P2X3 受体拮抗剂,其对人同源重组 hP2X3 和 hP2X2/3 的 IC50值分别是约 30 和 100-250 nM。

产品描述

Gefapixant is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.

体外活性

The IC50 of Gefapixant has been reported as ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors, potencies very similar to those reported for recombinant rat receptors, and it 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).

体内活性

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

动物实验

A rodent model often employs for assessing the potential for drug effect in osteoarthritis (OA) pain is based on the intraarticular injection of monoiodoacetate (mIOA) into one knee joint of the rat. To measure the effect of Gefapixant on the weight bearing laterality and apparent hyperalgesia, Gefapixant is given by intraplantar or oral administration to the rats, with different concentrations (6, 20, and 60 mg/kg) two times a day and continues up to a week[2].

Cas No.

1015787-98-0

分子式

C14H19N5O4S

分子量

353.4

别名

RO 4926219;MK-7264;AF219

储存和溶解度

H2O:Insoluble
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years