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S1RA {[allProObj[0].p_purity_real_show]}

货号:A451689 同义名: E-52862 Ambeed 开学季,买赠积分,赢豪礼

S1RA is a potent and selective sigma-1 receptor (σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).

S1RA 化学结构 CAS号:878141-96-9
S1RA 化学结构
CAS号:878141-96-9
S1RA 3D分子结构
CAS号:878141-96-9
S1RA 化学结构 CAS号:878141-96-9
S1RA 3D分子结构 CAS号:878141-96-9
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S1RA 纯度/质量文件 产品仅供科研

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S1RA 生物活性

描述 S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. Its activity extends moderately towards the human 5-HT2B receptor with a Ki of 328 nM. This selectivity profile is complemented by its antinociceptive capabilities in models of neuropathic pain, demonstrating efficacy in preventing both mechanical and cold hypersensitivity in mice treated with Oxaliplatin[1][2].
体内研究

In vivo, a single intraperitoneal (IP) dose of S1RA at 40 mg/kg leads to a significant reduction in pain responses induced by Allylisothiocyanate (AITC) in wild-type (WT) mice. Further demonstrating its analgesic potential, the same dosing regimen, administered once daily for 11 days starting 3 days before Oxaliplatin injection, effectively counters mechanical and cold hypersensitivity induced by the chemotherapy agent Oxaliplatin in mice[2].

体外研究

In cell-based assays, S1RA at a concentration of 100 µM over 4 hours can inhibit intracellular calcium responses in TRPA1-expressing HEK293 cells, illustrating its potential for modulating ion channel activities. It also impairs the formation of TRPA1–Sigma-1R complexes and reduces TRPA1 expression at the plasma membrane, which could underlie some of its therapeutic effects[2].

S1RA 参考文献

[1]Díaz JL, et al. Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). J Med Chem. 2012 Oct 11;55(19):8211-24.

[2]Aida Marcotti, et al. TRPA1 modulation by Sigma-1 receptor prevents oxaliplatin-induced painful peripheral neuropathy. Brain. 2023 Feb 13;146(2):475-491.

S1RA 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.82mL

2.96mL

1.48mL

29.64mL

5.93mL

2.96mL

S1RA 技术信息

CAS号878141-96-9
分子式C20H23N3O2
分子量 337.416
别名 E-52862
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 35 mg/mL(103.73 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

1M HCl: 50 mg/mL(148.19 mM),配合低频超声,并调节pH至1

动物实验配方
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