Gefapixant citrate  (Synonyms: MK-7264 citrate; AF-219 citrate)

Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC₅₀ values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis^[1][2][3].

Gefapixant citrate 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Gefapixant citrate (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)^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

545.52

C₂₀H₂₇N₅O₁₁S

2310299-91-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Anthony P. Ford, et al. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Front Cell Neurosci. 2013; 7: 267.  [Content Brief]

  [2]. Ford AP, In pursuit of P2X3 antagonists: novel therapeutics for chronic pain and afferent sensitization. Purinergic Signal. 2012 Feb;8(Suppl 1):3-26.  [Content Brief]

  [3]. Martin Nguyen A, et al. Validation of a visual analog scale for assessing cough severity in patients with chronic cough. Ther Adv Respir Dis. 2021 Jan-Dec;15:17534666211049743.  [Content Brief]