| 产品描述： | PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models |
| 靶点： |
A2A adenosine;AdenosineReceptor |
| 体内研究： |
PD 117519 (2-10 mg/kg; oral administration; 16-24 hours; male beagle dogs) treatment produces significant hemodynamic changes at Tmax (4 hours) follows by acute coronary vascular injury that is evident at 16 hours postdosing.Treatment with 2 or 10 mg/kg of PD 117519 produces significant increases in mean heart rate and decreases in mean indirectsystolic blood pressure at time of highest drug exposure, 4 hours postdosing. Animal Model: 24 male beagle dogs (8-12 months old) Dosage: 2 mg/kg or 10 mg/kg Administration: Oral administration; 16 hours and 24 hours Result: Increased in mean heart rate and decreased in mean indirectsystolic blood pressure at time of highest drug exposure. Induced acute coronary arteriopathy. The endothelium also appears injured. |
| 参考文献： |
1. Reynolds DL, et al. Liquid chromatographic analysis of the adenosine agonist PD 117519 in dog plasma. J Pharm Biomed Anal. 1991;9(4):345-9. 2. Tobin GA, et al. The role of eNOS phosphorylation in causing drug-induced vascular injury. Toxicol Pathol. 2014 Jun;42(4):709-24. 3. Enerson BE, et al. Acute drug-induced vascular injury in beagle dogs: pathology and correlating genomic expression. Toxicol Pathol. 2006;34(1):27-32. |
| 溶解性： |
Soluble in DMSO |
| 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 |
2.608 ml |
13.041 ml |
26.082 ml |
| 5 mM |
0.522 ml |
2.608 ml |
5.216 ml |
| 10 mM |
0.261 ml |
1.304 ml |
2.608 ml |
| 50 mM |
0.052 ml |
0.261 ml |
0.522 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京