Gefapixant(AF-219,MK-7264)

Cas No.:	1015787-98-0
Chemical Name:	Gefapixant
Synonyms:	RO-4926219;EOS-6104;EOS-61047;Gefapixant;Gefapixant(AF-219,MK-7264);5-(2,4-DiaMino-pyriMidin-5-yloxy)-4-isopropyl-2-Methoxy-benzenesulfonaMide;RO4926219;6K6L7E3F1L;RG1646;R1646;5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzene-1-sulfonamide;C14H19N5O4S;5-(2,4-diaminopyrimidin-5-yl)oxy-2-methoxy-4-propan-2-ylbenzenesulfonamide;5-[2,4-bis(azanyl)pyrimidin-5-yl]oxy-2-methoxy-4-propan-2-yl-benzenesulfonamide;Benzenesulfonamide, 5-((2,4-diamino-5-pyrimidinyl)oxy)-2-methoxy-4-(1-methylethyl)-;Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimid
SMILES:	S(C1C([H])=C(C(=C([H])C=1OC([H])([H])[H])C([H])(C([H])([H])[H])C([H])([H])[H])OC1=C([H])N=C(N([H])[H])N=C1N([H])[H])(N([H])[H])(=O)=O
Formula:	C14H19N5O4S
M.Wt:	353.3968
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC 50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
In Vivo:	In an adjuvant-induced rthritis model in rat (7d following intraplantar administration of complete Freund's adjuvant), AF-353 produces dose-dependent antihyperalgesia in weight-bearing asymmetry and von Frey filament mechanical tests; magnitude of effect is compared with that of the NSAID naproxen. In a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate), Gefapixant (7d bid, orally; right) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses[2].
In Vitro:	The aryloxy-pyrimidinediamine, Gefapixant (AF-219) is an orally active small molecule antagonist at human P2X3-containing receptors. 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)[1].