| 产品描述： | IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo[1] |
| 靶点： |
ETB:1.3 nM (IC50);ETA:94 nM (IC50) |
| 体外研究： |
IRL 2500 also decreases the IRL 1620-mediated enhances renal vascular resistance (RVR) in the anesthetized rat[1]. IRL 2500 (intravenous?injection;10 mg/kg) suppresses the initial transient reduction in mean arterial pressure (MAP) induced by the ETB-selective agonist IRL 1620 in rats. IRL 2500 (intravenous?injection;10 mg/kg) pre-treatment obviously reduces the initial vasodepressor response to endothelin-1 (ET-1) and IRL 1620, however, it does not alter the secondary and sustained pressor response to these agonists. |
| 体内研究： |
IRL 2500 (intravenous injection;10 mg/kg) inhibits the initial transient decrease in mean arterial pressure (MAP) induced by the ETB-selective agonist IRL 1620 in rats, IRL 2500 also attenuates the IRL 1620-mediated increase in renal vascular resistance (RVR) in the anesthetized rat. IRL 2500 (intravenous injection;10 mg/kg) pre-reatment significantly reduces the initial vasodepressor response to endothelin-1 (ET-1) and IRL 1620, however, it is not alters the secondary and sustained pressor response to these agonists |
| 参考文献： |
1.Balwierczak JL, et al. Characterization of a potent and selective endothelin-B receptor antagonist, IRL 2500.J Cardiovasc Pharmacol. 1995;26 Suppl 3:S393-6. 2.Webb RL, et al. Effects of the ETB-selective antagonist IRL 2500 in conscious spontaneously hypertensive and Wistar-Kyoto rats.J Cardiovasc Pharmacol. 1995;26 Suppl 3:S389-92. |
| 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 |
1.743 ml |
8.716 ml |
17.431 ml |
| 5 mM |
0.349 ml |
1.743 ml |
3.486 ml |
| 10 mM |
0.174 ml |
0.872 ml |
1.743 ml |
| 50 mM |
0.035 ml |
0.174 ml |
0.349 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