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Gefapixant

Chemical Structure : Gefapixant

CAS No.: 1015787-98-0

Gefapixant (AF-219, MK-7264)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 353.397
Formula C14H19N5O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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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