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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-P2X Receptor-Gefapixant
Gefapixant

Chemical Structure : Gefapixant

CAS No.: 1015787-98-0

Gefapixant (AF-219, MK-7264)

货号: PC-61379Not For Human Use, Lab Use Only.

Gefapixant (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).

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10 mg ¥1280 In stock
25 mg ¥1980 In stock
50 mg ¥2980 In stock
100 mg ¥4580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Gefapixant (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 353.397
分子式 C14H19N5O4S
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

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.

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