Gefapixant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Gefapixant (AF-219, MK-7264) 是一种口服有效的小分子 P2X3 含受体拮抗剂，IC50 为 30 nM（hP2X3 同源三聚体）和 100-250 nM（hP2X2/3 异源三聚体）。

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); 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); markedly and significantly reduced objective cough frequency in clinical trials.Asthma Phase 2 Clinical.

Gefapixant 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).

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

AF-219 | MK-7264

Membrane Transporter/Ion Channel

P2X Receptor

recombinanthP2X3homotrimers|hP2X2/3heterotrimericreceptors

Inflammation/Immunology

Asthma

1015787-98-0

353.397

C14H19N5O4S

>98% (HPLC)

DMSO: 10 mM （(< 1 mg/ml )

O=S(C1=CC(OC2=CN=C(N)N=C2N)=C(C(C)C)C=C1OC)(N)=O

5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzene-1-sulfonamide

(-20℃)

With Ice Pack

≥ 2 years