化学信息：
| 化学名 | 4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine |
|
| 简称 | S1RA | |
| 别名 |
E-52862, E52862, E 52862 |
|
| 中文名 | N/A | |
| 化学式 | C20H23N3O2 | |
| 分子量 | 337.42 | |
| CAS号 | 878141-96-9 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO40mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入1.48ml DMSO，或者每3.37mg加入1ml DMSO，配制成10mM溶液。SD2393-10mM用DMSO配制。 |
生物信息：
| 产品描述 | S1RA (E-52862) is a potent and selective sigma-1 receptor (σ1R, Ki=17nM) antagonist, showed good selectivity against σ2R (Ki>1000nM). | ||||
| 信号通路 | GPCR & G Protein | ||||
| 靶点 | σ1R | σ2R | － | － | － |
| IC50 | 17nM (Ki) | >1000nM (Ki) | － | － | － |
| 体外研究 | S1RA behaved as a highly selective σ1 receptor antagonist. It showed high affinity for human (Ki=17nM) and guinea pig (Ki=23.5nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki>1000nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki=328nM) and antagonistic activity, with very low potency (IC50=4700nM) was found at the human 5-HT2B receptor. S1RA showed no significant affinity (Ki>1μM or % inhibition at 1μM <50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes). | ||||
| 体内研究 | Control (non-operated) and nerve-injured mice received a single or repeated (twice daily for 12 days) i.p. administration of S1RA at 25mg·kg/L, the same dose used for the assessment of behavioural hypersensitivity in the chronic treatment study. Acute treatment was given on day 12 post-surgery and repeated treatment with S1RA started the day of surgery, as in the behavioural studies. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited only the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuated the lifting/licking behavior. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SD2393-10mM | S1RA (Sigma Receptor拮抗剂) | 10mM×0.2ml |
| SD2393-5mg | S1RA (Sigma Receptor拮抗剂) | 5mg |
| SD2393-25mg | S1RA (Sigma Receptor拮抗剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
