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S1RA

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Chemical Structure| 878141-96-9 同义名 : E-52862
CAS号 : 878141-96-9
货号 : A451689
分子式 : C20H23N3O2
纯度 : 99%
分子量 : 337.416
MDL号 : MFCD25976945
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：
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].
实验方案
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
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.