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S1RA HCl

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Chemical Structure| 1265917-14-3 同义名 : E-52862 hydrochloride;S1RA (hydrochloride);P 027;E-52862;S1RA hydrochloride
CAS号 : 1265917-14-3
货号 : A242234
分子式 : C20H24ClN3O2
纯度 : 99%+
分子量 : 373.877
MDL号 : MFCD27963345
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：
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].
实验方案
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
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.