| 靶点: |
pEC50: 7.4 |
| 体内研究: |
GSK726701A has good pharmacokinetic file in rat, dog and monkey. GSK726701A has robust activity in a range of animal models of inflammatory and neuropathic pain GSK726701A demonstrates a time-dependant, full reversal of CCI-induced mechanical allodynia at 3mg/kg, equivalent to the clinical gold standard gabapentin (30mg/kg). GSK726701A has an ED50 of 0.2mg/kg in the FCA acute rat model of inflammatory pain. |
| 参考文献: |
1. Healy MP, et al. Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1892-1896. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.362 ml |
11.808 ml |
23.617 ml |
| 5 mM |
0.472 ml |
2.362 ml |
4.723 ml |
| 10 mM |
0.236 ml |
1.181 ml |
2.362 ml |
| 50 mM |
0.047 ml |
0.236 ml |
0.472 ml |
|
| 注意: |
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