Gefapixant
产品说明书
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同义名 : | MK-7264;AF-219 |
| CAS号 : | 1015787-98-0 | |
| 货号 : | A503454 | |
| 分子式 : | C14H19N5O4S | |
| 纯度 : | 99% | |
| 分子量 : | 353.397 | |
| MDL号 : | MFCD24539325 | |
| 存储条件： |
Pure form Keep in dark place,Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 4 mg/mL(11.32 mM)，配合低频超声，并调节pH至5-6，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Gefapixant is an orally effective antagonist of P2X3R, with an IC50 value of approximately 30 nM against recombinant homotrimeric hP2X3, and an IC50 value ranging from 100-250 nM against the heterotrimeric hP2X2/3 receptor. Gefapixant does not inhibit receptors containing non-P2X3 subunits, including recombinant homotrimers hP2X1, hP2X2, hP2X4, rP2X5, and hP2X7. Gefapixant is useful for research into chronic cough and knee osteoarthritis[1][2][3]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02612623 | Refractory Chronic Cough | Phase 2 | Completed | - | United States, California ... 展开 >> Afferent Investigative Site Mission Viejo, California, United States Afferent Investigative Site San Jose, California, United States United States, Colorado Afferent Investigative Site Colorado Springs, Colorado, United States United States, Florida Afferent Investigative Site Largo, Florida, United States United States, North Carolina Afferent Investigative Site Charlotte, North Carolina, United States United States, Oklahoma Afferent Investigative Site Tulsa, Oklahoma, United States United States, Texas Afferent Investigative Site Dallas, Texas, United States Afferent Investigative Site San Antonio, Texas, United States United States, Washington Afferent Investigative Site Bellevue, Washington, United States United States, Wisconsin Afferent Investigative Site Greenfield, Wisconsin, United States 收起 << |
| NCT01554579 | Osteoarthritis of the Knee | Phase 2 | Completed | - | - |
| NCT01554579 | - | Completed | - | - | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.83mL 0.57mL 0.28mL |
14.15mL 2.83mL 1.41mL |
28.30mL 5.66mL 2.83mL |
| 参考文献 |
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