Gefapixant citrate
Based on 2 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.23%
- CAS No.: 2310299-91-1
- Formula: C20H27N5O11S
- Molecular Weight:545.52
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Gefapixant citrate
MoreAll P2X Receptor Isoforms
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Biological Activity
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P2X3 Receptor |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2310299-91-1
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Appearance Solid
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Molecular Weight 545.52
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Formula C20H27N5O11S
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Color White to off-white
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SMILES
O=C(CC(C(O)=O)(CC(O)=O)O)O.O=S(N)(C1=C(OC)C=C(C(C)C)C(OC2=CN=C(N)N=C2N)=C1)=O
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Synonyms
MK-7264 citrate; AF-219 citrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Mol Ther
2025 Feb 5;33(2):771-785. PMID: 39960544 -
Function (Oxf)
Topical ATP Application in the Peripheral Swallowing-Related Regions Facilitates Triggering of the Swallowing Reflex Involving P2X3 Receptors. [Abstract]2025 Mar 24;6(2):zqaf010. PMID: 40042973
Solvent & Solubility
DMSO : 350 mg/mL (641.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8331 mL | 9.1656 mL | 18.3311 mL | 45.8278 mL |
| 5 mM | 0.3666 mL | 1.8331 mL | 3.6662 mL | 9.1656 mL | |
| 10 mM | 0.1833 mL | 0.9166 mL | 1.8331 mL | 4.5828 mL | |
| 15 mM | 0.1222 mL | 0.6110 mL | 1.2221 mL | 3.0552 mL | |
| 20 mM | 0.0917 mL | 0.4583 mL | 0.9166 mL | 2.2914 mL | |
| 25 mM | 0.0733 mL | 0.3666 mL | 0.7332 mL | 1.8331 mL | |
| 30 mM | 0.0611 mL | 0.3055 mL | 0.6110 mL | 1.5276 mL | |
| 40 mM | 0.0458 mL | 0.2291 mL | 0.4583 mL | 1.1457 mL | |
| 50 mM | 0.0367 mL | 0.1833 mL | 0.3666 mL | 0.9166 mL | |
| 60 mM | 0.0306 mL | 0.1528 mL | 0.3055 mL | 0.7638 mL | |
| 80 mM | 0.0229 mL | 0.1146 mL | 0.2291 mL | 0.5728 mL | |
| 100 mM | 0.0183 mL | 0.0917 mL | 0.1833 mL | 0.4583 mL |
Gefapixant citrate Related Classifications
HY-101588A Related Classifications
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