For research use only. Not for therapeutic Use.
Gefapixant 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 can be used for the research of chronic cough and knee osteoarthritis[1][2][3].
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)[1].
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)[2].
| Catalog Number | I019976 |
| CAS Number | 1015787-98-0 |
| Synonyms | 5-(2,4-diaminopyrimidin-5-yl)oxy-2-methoxy-4-propan-2-ylbenzenesulfonamide |
| Molecular Formula | C14H19N5O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C14H19N5O4S/c1-7(2)8-4-10(22-3)12(24(17,20)21)5-9(8)23-11-6-18-14(16)19-13(11)15/h4-7H,1-3H3,(H2,17,20,21)(H4,15,16,18,19) |
| InChIKey | HLWURFKMDLAKOD-UHFFFAOYSA-N |
| SMILES | CC(C)C1=CC(=C(C=C1OC2=CN=C(N=C2N)N)S(=O)(=O)N)OC |
| Reference | [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. [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. [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. |
