Gefapixant citrate

Modify Date: 2024-01-03 03:18:07

Gefapixant citrate Structure
Gefapixant citrate structure
Common Name Gefapixant citrate
CAS Number 2310299-91-1 Molecular Weight 545.52
Density N/A Boiling Point N/A
Molecular Formula C20H27N5O11S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Gefapixant 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].

 Names

Name Gefapixant citrate

 Gefapixant citrate Biological Activity

Description 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].
Related Catalog
Target

IC50: ~30 nM (recombinant hP2X3 homotrimers), 100-250 nM (hP2X2/3 heterotrimeric receptors)[1].

In Vitro 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].
In Vivo 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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C20H27N5O11S
Molecular Weight 545.52