S1RA 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 (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]. |
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 |
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 |