| 产品描述： | Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA |
| 靶点： |
IC50: 0.055 nM (ETA) |
| 体内研究： |
Atrasentan hydrochloride (ABT-627 hydrochloride) (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats. Aatrasentan (ABT-627, 10 mg/kg, i.p.) inhibits the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model |
| 参考文献： |
1. Yuyama H, et al. Superiority of YM598 over atrasentan as a selective endothelin ETA receptor antagonist. Eur J Pharmacol. 2004 Sep 13;498(1-3):171-7. 2. Banerjee S, et al. In vitro and in vivo molecular evidence for better therapeutic efficacy of ABT-627 combination in prostate cancer. Cancer Res. 2007 Apr 15;67(8):3818-26. 3. Weiss J, et al. Interaction potential of the endothelin-A receptor antagonist atrasentan with drug transporters and drug-metabolising enzymes assessed in vitro. Cancer Chemother Pharmacol. 2011 Oct;68(4):1093-8. |
| 溶解性： |
DMSO : 28.57 mg/mL (52.22 mM; Need ultrasonic) H2O : 0.5 mg/mL (0.91 mM; ultrasonic and warming and adjust pH to 4 with HCl and heat to 60°C) 0.1 M HCL : < 1 mg/mL (ultrasonic;warming;adjust pH to 1 with HCl;heat to 60°C) (insoluble) |
| 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 |
1.828 ml |
9.139 ml |
18.279 ml |
| 5 mM |
0.366 ml |
1.828 ml |
3.656 ml |
| 10 mM |
0.183 ml |
0.914 ml |
1.828 ml |
| 50 mM |
0.037 ml |
0.183 ml |
0.366 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