- 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)
- 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℃
- 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。
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
