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S1RA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
S1RA图片
CAS NO:878141-96-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
S1RA(E-52862) 是一种有效的选择性 sigma-1 receptor(σ1R, Ki=17 nM) 拮抗剂,对 σ2R (Ki >1000 nM) 表现出良好的选择性。
Cas No.878141-96-9
别名E-52862
化学名4-(2-((5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yl)oxy)ethyl)morpholine
Canonical SMILESCC1=CC(OCCN2CCOCC2)=NN1C3=CC4=CC=CC=C4C=C3
分子式C20H23N3O2
分子量337.42
溶解度≥ 10.35mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

S1RA is a potent and selective antagonist of σ1 receptor (σ1R) with Ki value of 17nM [1].

S1RA is the first σ1 receptor antagonist with potent antinociceptive activities in various pain models. In the binding assay, S1RA shows good affinity to human σ1 receptor transfected in HEK293 membranes with Ki value of 17nM. The Ki value for guinea pig brain membrane σ1 receptor is higher than 1μM. S1RA also shows no significant affinity to another 170 molecular targets including receptors, ion channels and enzymes [1, 2].

In the mouse tests, S1RA exhibits potent analgesic effects on capsaicin-induced mechanical hypersensitivity and formalin-induced pain. Besides that, S1RA inhibits both mechanical allodynia and thermal hypersensitivity with ED50 values of 23.4mg/kg and 18.8mg/kg in the partial sciatic nerve ligation model in mice [1].

References:
[1] Diaz J L, Cuberes R, Berrocal J, et al. Synthesis and Biological Evaluation of the 1-Arylpyrazole Class of σ1 Receptor Antagonists: Identification of 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1 H-pyrazol-3-yloxy] ethyl} morpholine (S1RA, E-52862). Journal of medicinal chemistry, 2012, 55(19): 8211-8224.
[2] Wunsch B. The σ1 Receptor Antagonist S1RA Is a Promising Candidate for the Treatment of Neurogenic PainJ. Journal of medicinal chemistry, 2012, 55(19): 8209-8210.