| 产品描述： | ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions |
| 靶点： |
TRP Channel |
| 体外研究： |
ASP7663 concentration dependently increases intracellular Ca2+ concentration in human, rat, and mouse TRPA1 expressed in HEK293 cells in a similar manner, with respective EC50 values (95% confidence interval [CI]) of 0.51 (0.40–0.66), 0.54 (0.41–0.72), and 0.50 (0.41–0.63) μmol/L. ASP7663 concentration-dependently stimulates 5-HT release from QGP-1 cells, a lineage of TRPA1-expressing EC cells, with an EC50 value of 72.5 (52.6–99.9) μmol/L |
| 体内研究： |
ASP7663 significantly improves the loperamide-induced delay in colonic transit in mice. ASP7663 (orally, 0.3 and 1 mg/kg) significantly shortens the prolonged bead expulsion time caused by loperamide. ASP7663 (orally, 1 and 3 mg/kg) exhibits inhibitory effects on colorectal distension in rat. Animal Model: CRD model (colorectal distension in rat). Dosage: 1 and 3 mg/kg. Administration: Orally. Result: Significantly reduced the number of abdominal contractions evoked during CRD at pressures of 30, 45, and 60 mmHg. ASP7663 also reduced the number of abdominal contractions by intravenous treatment. |
| 参考文献： |
1. Ryosuke Kojima, et al. Effects of Novel TRPA1 Receptor Agonist ASP7663 in Models of Drug-Induced Constipation and Visceral Pain. Eur J Pharmacol. 2014 Jan 15;723:288-93. 2. Yao Lu, et al. Transient Receptor Potential Ankyrin 1 Activation Within the Cardiac Myocyte Limits Ischemia-reperfusion Injury in Rodents. Anesthesiology. 2016 Dec;125(6):1171-1180. |
| 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 |
3.799 ml |
18.993 ml |
37.985 ml |
| 5 mM |
0.76 ml |
3.799 ml |
7.597 ml |
| 10 mM |
0.38 ml |
1.899 ml |
3.799 ml |
| 50 mM |
0.076 ml |
0.38 ml |
0.76 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