2310299-91-1
2310299-91-1 structure
- Name: Gefapixant citrate
- Chemical Name: Gefapixant citrate
- CAS Number: 2310299-91-1
- Molecular Formula: C20H27N5O11S
- Molecular Weight: 545.52
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel P2X Receptor
- Create Date: 2022-08-10 11:21:55
- Modify Date: 2024-01-03 03:18:07
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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].
| Name | Gefapixant citrate |
|---|
| 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]. |
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| 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 |
| Molecular Formula | C20H27N5O11S |
|---|---|
| Molecular Weight | 545.52 |