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S1RA HCl {[allProObj[0].p_purity_real_show]}

货号:A242234 同义名: E-52862 hydrochloride;S1RA (hydrochloride) Ambeed 开学季,买赠积分,赢豪礼

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

S1RA HCl 化学结构 CAS号:1265917-14-3
S1RA HCl 化学结构
CAS号:1265917-14-3
S1RA HCl 3D分子结构
CAS号:1265917-14-3
S1RA HCl 化学结构 CAS号:1265917-14-3
S1RA HCl 3D分子结构 CAS号:1265917-14-3
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S1RA HCl 纯度/质量文件 产品仅供科研

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S1RA HCl 生物活性

描述 S1RA hydrochloride, the orally active form of S1RA, retains high selectivity for the σ1R over σ2R, with Ki values significantly greater than 1000 nM for the latter. Despite its moderate antagonism of the human 5-HT2B receptor (with an IC50 of 4.7 μM), S1RA hydrochloride's primary pharmacological effect is mitigating neuropathic pain and preventing activity-induced spinal sensitization[1][2].
体内研究

S1RA hydrochloride has shown efficacy in various pain models, significantly inhibiting formalin-induced nociception, capsaicin-induced mechanical hypersensitivity, and sciatic nerve injury-induced mechanical and thermal hypersensitivity in mice, across a wide dose range through both intraperitoneal and oral administration[1].

体外研究

S1RA hydrochloride distinguishes itself as a highly selective antagonist for the sigma-1 receptor (σ1R), with strong affinity indicated by Ki values of 17 nM and 23.5 nM for human and guinea pig σ1Rs, respectively. Its affinity extends to the human σ2R, albeit at a much higher Ki value of 9.3 μM, demonstrating its selectivity towards σ1R. Additionally, S1RA hydrochloride targets the human 5-HT2B receptor, with a Ki value of 328 nM and an IC50 value of 4.7 μM, indicating a moderate antagonistic activity[1].

S1RA HCl 参考文献

[1]Romero L, 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 Aug;166(8):2289-306.

[2]Vidal-Torres A, et al. Effects of the selective sigma-1 receptor antagonist S1RA on formalin-induced pain behavior and neurotransmitter release in the spinal cord in rats. J Neurochem. 2014 Jan 3.

S1RA HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.67mL

0.53mL

0.27mL

13.37mL

2.67mL

1.34mL

26.75mL

5.35mL

2.67mL

S1RA HCl 技术信息

CAS号1265917-14-3
分子式C20H24ClN3O2
分子量 373.877
别名 E-52862 hydrochloride;S1RA (hydrochloride);P 027;E-52862;S1RA hydrochloride
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(280.84 mM),配合低频超声助溶,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

H2O: 15 mg/mL(40.12 mM),配合低频超声助溶

动物实验配方
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