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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.23%
- CAS 番号: 2310299-91-1
- 分子式: C20H27N5O11S
- 分子量:545.52
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Gefapixant citrate
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生物活性
製品説明
IC50 & Target
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P2X3 Receptor |
体外実験
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. .
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2310299-91-1
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性状 Solid
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分子量 545.52
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分子式 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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別名
MK-7264 citrate; AF-219 citrate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 |
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| 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 関連分類
HY-101588A 関連分類
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