| 产品描述： | RO-3 is a potent, CNS-penetrant, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7) |
| 靶点： |
pIC50: 5.9 (human homomultimeric P2X3 receptor); 7.0 (human heteromultimeric P2X2/3 receptor) |
| 体内研究： |
In a guinea pig ureter-afferent nerve preparation, and mouse bladder-pelvic nerve preparation, RO-3 dose-dependently reduces afferent nerve activity induced by distension or α,β-meATP. RO-3 has activity in several rodent models of pain, as well as in cystometry models optimized to measure various parameters associated with sensory regulation of the micturition reflex. RO-3 has moderate to high metabolic stability in rat and human hepatocytes and liver microsomes, and is highly permeable, orally bioavailable (14%), and has a reasonable in vivo plasma half-life (t1/2=0.41 h) in rats |
| 参考文献： |
1. Ford AP, et al. Purinoceptors as therapeutic targets for lower urinary tract dysfunction. Br J Pharmacol. 2006;147 Suppl 2(Suppl 2):S132-S143. |
| 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 |
3.307 ml |
16.536 ml |
33.072 ml |
| 5 mM |
0.661 ml |
3.307 ml |
6.614 ml |
| 10 mM |
0.331 ml |
1.654 ml |
3.307 ml |
| 50 mM |
0.066 ml |
0.331 ml |
0.661 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