Gefapixant citrate

Chemical Structure : Gefapixant citrate

CAS No.: 2310299-91-1

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货号: PC-25643Not For Human Use, Lab Use Only.

Gefapixant citrate (AF-219, MK-7264) is an orally active, small molecule antagonist of P2X3-containing receptor with IC50 of 30 nM (hP2X3 homotrimer) and 100-250 nM (hP2X2/3 heterotrimer).

规格	价格	库存
10 mg	￥780	In stock
25 mg	￥1280	In stock
50 mg	￥1980	In stock
100 mg		Get quote

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生物&药学活性

Gefapixant citrate (AF-219, MK-7264) is an orally active, small molecule antagonist of P2X3-containing receptor with IC50 of 30 nM (hP2X3 homotrimer) and 100-250 nM (hP2X2/3 heterotrimer).
Gefapixant (AF-219, MK-7264) displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC50 >10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5 and hP2X7 channels).
Gefapixant (AF-219, MK-7264) markedly and significantly reduced objective cough frequency in clinical trials.

物理化学性质&存储条件

分子量	545.52
分子式	C20H27N5O11S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzene-1-sulfonamide citrate

参考文献

1. Abdulqawi R, et al. Lancet. 2015 Mar 28;385(9974):1198-205.

2. Ford AP, et al. Front Cell Neurosci. 2013 Dec 19;7:267.