货号:A242234
同义名:
E-52862 hydrochloride; S1RA (hydrochloride)
S1RA HCl is a potent and selective sigma-1 receptor (σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).
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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]. |
Animal study | 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]. |
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 |
CAS号 | 1265917-14-3 |
分子式 | C20H24ClN3O2 |
分子量 | 373.88 |
SMILES Code | CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3.[H]Cl |
MDL No. | MFCD27963345 |
别名 | E-52862 hydrochloride; S1RA (hydrochloride); P 027; E-52862; S1RA hydrochloride |
运输 | 蓝冰 |
InChI Key | SHRYQZBTQDMGLZ-UHFFFAOYSA-N |
Pubchem ID | 50914801 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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