| 产品描述： | S1RA (E-52862)是一种选择性sigma-1 receptor (σ1R)拮抗剂，对人源σ1受体的结合亲和力Ki为17 nM |
| 靶点： |
σ1R:17 nM(Ki);Sigmareceptor |
| 体外研究： |
S1RA behaves as a highly selective σ1 receptor antagonist. It shows high affinity for human (Ki= 17 nM) and guinea pig (Ki= 23.5 nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). It has moderate affinity (Ki= 328 nM) and antagonistic activity, with very low potency (IC50= 4700 nM) against human 5-HT2B receptor. S1RA shows no significant affinity (Ki > 1 µM or % inhibition at 1 µM < 50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes) |
| 体内研究： |
S1RA crosses the blood-brain barrier and binds to σ1 receptors in the CNS |
| 参考文献： |
1. L Romero, et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012, 166(8): 2289–2306. |
| 溶解性： |
Soluble in DMSO、Ethanol、H2O |
| 保存条件： |
-20°C |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.964 ml |
14.819 ml |
29.637 ml |
| 5 mM |
0.593 ml |
2.964 ml |
5.927 ml |
| 10 mM |
0.296 ml |
1.482 ml |
2.964 ml |
| 50 mM |
0.059 ml |
0.296 ml |
0.593 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