Powder: -20°C for 3 years | In solvent: -80°C for 1 year
S1RA hydrochloride (E-52862 hydrochloride) 是一种有效且特异性的 sigma-1受体拮抗剂,Ki 为17nM,对 σ2R 具有良好的选择性,Ki 值大于 1000 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 392 | 现货 | ||
2 mg | ¥ 563 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,370 | 现货 | ||
25 mg | ¥ 2,890 | 现货 | ||
50 mg | ¥ 4,360 | 现货 | ||
100 mg | ¥ 6,190 | 现货 | ||
500 mg | ¥ 12,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 976 | 现货 |
产品描述 | S1RA hydrochloride (E-52862 hydrochloride) is an effective and specific sigma-1 receptor(σ1R, Ki: 17 nM) antagonist, and has good selectivity against σ2R (Ki > 1000 nM). |
靶点活性 | σ1:17 nM |
体外活性 | S1RA showed high affinity for the guinea pig (Ki: 23.5 nM) and human (Ki: 17 nM) σ1 receptors but no marked affinity for the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki: 328 nM) and antagonistic activity with very low potency (IC50: 4700 nM) were found at the human 5-HT2B receptor. S1RA showed a low affinity (Ki > 1 μM, IC50>1 μM) for other additional 170 targets (transporters, receptors, ion channels and enzymes). |
体内活性 | Control (non-operated) and nerve-injured mice received a single or repeated (b.i.d, for 12 days) S1RA (25 mg/kg, i.p.), the same dose used for the assessment of behavioral hypersensitivity in the chronic treatment study. In the behavioral studies, acute treatment was given on day 12 post-surgery and repeated treatment with S1RA started the day of surgery. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited only the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuated the lifting/licking behavior. |
别名 | 4-[2-[[5-甲基-1-(2-萘基)-1H-吡唑-3-基]氧基]乙基]吗啉盐酸盐(1:1), E-52862 hydrochloride |
分子量 | 373.87 |
分子式 | C20H24ClN3O2 |
CAS No. | 1265917-14-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 57 mg/mL
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
S1RA hydrochloride 1265917-14-3 GPCR/G Protein Sigma receptor Inhibitor E 52862 E 52862 Hydrochloride 4-[2-[[5-甲基-1-(2-萘基)-1H-吡唑-3-基]氧基]乙基]吗啉盐酸盐(1:1) E52862 S1RA E-52862 E-52862 Hydrochloride E-52862 hydrochloride inhibit S1RA Hydrochloride S-1RA hydrochloride Sigma Receptor E52862 Hydrochloride inhibitor