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S1RA Sale

(Synonyms: E-52862) 目录号 : GC10407

A σ1 receptor antagonist

S1RA Chemical Structure

Cas No.:878141-96-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,153.00
现货
5mg
¥2,174.00
现货
10mg
¥2,804.00
现货
50mg
¥8,264.00
现货

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Sample solution is provided at 25 µL, 10mM.

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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] Díaz 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.

Chemical Properties

Cas No. 878141-96-9 SDF
别名 E-52862
化学名 4-(2-((5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yl)oxy)ethyl)morpholine
Canonical SMILES CC1=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
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.9637 mL 14.8183 mL 29.6367 mL
5 mM 0.5927 mL 2.9637 mL 5.9273 mL
10 mM 0.2964 mL 1.4818 mL 2.9637 mL
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