Gefapixant
Gefapixant (MK-7264) 是一个口服的、P2X3 受体活性拮抗剂，其对人同源重组 hP2X3 和 hP2X2/3 的 IC50 值分别是 ~30 nM 和 100-250 nM。
For research use only. We do not sell to patients.
化学信息
| 名称 | Gefapixant |
|---|---|
| Iupac 化学名称 | 5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzene-1-sulfonamide |
| 同义词 | Gefapixant ; MK-7264 ; MK 7264 ; MK7264 ; AF-219 ; AF219 ; AF 219 ; RO4926219 ; RO-4926219 ; RO 4926219 ; |
| 分子式 | C14H19N5O4S |
| 分子量 | 353.39 |
| Smile | O=S(C1=CC(OC2=CN=C(N)N=C2N)=C(C(C)C)C=C1OC)(N)=O |
| InChiKey | HLWURFKMDLAKOD-UHFFFAOYSA-N |
| 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) |
| Cas号 | 1015787-98-0 |
| Related CAS | 1015787-98-0 |
订购信息
| Packaging | 价格 | Availability | 纯度 | Shipping Time |
|---|---|---|---|---|
| Bulk | 询价 | 询价 | 询价 |
| Formulation | 类白色至白色固体 |
|---|---|
| 纯度 | 98% |
| 存储 | 短期可在0-4度保存，数天至数月；长期可在-20度保存三年。 |
| 可溶性 | 可溶于DMSO |
| Handling | Avoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation. |
| 运输条件 | 可在常温下运输 |
| HS Code |
| Targets | P2X3 Antagonist |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Wang J, Wang Y, Cui WW, Huang Y, Yang Y, Liu Y, Zhao WS, Cheng XY, Sun WS, Cao P, Zhu MX, Wang R, Hattori M, Yu Y. Druggable negative allosteric site of P2X3 receptors. Proc Natl Acad Sci U S A. 2018 May 8;115(19):4939-4944. doi: 10.1073/pnas.1800907115. Epub 2018 Apr 19. PubMed PMID: 29674445; PubMed Central PMCID: PMC5948998.
2: Burnstock G. The therapeutic potential of purinergic signalling. Biochem Pharmacol. 2018 May;151:157-165. doi: 10.1016/j.bcp.2017.07.016. Epub 2017 Jul 21. Review. PubMed PMID: 28735873.
3: Sheridan C. Merck stakes out 'irritable' neuron territory with $1.25 billion. Nat Biotechnol. 2016 Sep 8;34(9):900. doi: 10.1038/nbt0916-900. PubMed PMID: 27606448.
4: Abdulqawi R, Dockry R, Holt K, Layton G, McCarthy BG, Ford AP, Smith JA. P2X3 receptor antagonist (AF-219) in refractory chronic cough: a randomised, double-blind, placebo-controlled phase 2 study. Lancet. 2015 Mar 28;385(9974):1198-205. doi: 10.1016/S0140-6736(14)61255-1. Epub 2014 Nov 25. PubMed PMID: 25467586.
5: Morice AH. Developing antitussives the clinician's pipeline-what do we need? J Thorac Dis. 2014 Oct;6(Suppl 7):S735-8. doi: 10.3978/j.issn.2072-1439.2014.08.40. Review. PubMed PMID: 25383208; PubMed Central PMCID: PMC4222922.
6: Ochoa-Cortes F, Liñán-Rico A, Jacobson KA, Christofi FL. Potential for developing purinergic drugs for gastrointestinal diseases. Inflamm Bowel Dis. 2014 Jul;20(7):1259-87. doi: 10.1097/MIB.0000000000000047. Review. PubMed PMID: 24859298; PubMed Central PMCID: PMC4340257.
7: Ford AP, Undem BJ. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Front Cell Neurosci. 2013 Dec 19;7:267. doi: 10.3389/fncel.2013.00267. Review. PubMed PMID: 24391544; PubMed Central PMCID: PMC3867694.
