CAS:224177-60-0Siramesine hydrochloride

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Synonyms: Lu 28-179 HCl

Siramesine HCl is an agonist of sigma-2 receptor which can trigger cell death and exhibit anticancer activity.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

224177-60-0

储存条件

分子式

C30H32ClFN2O

运输

蓝冰

分子量

491.04

别名

Lu 28-179 HCl

溶解度

动物实验配方

生物活性

描述Sigma receptors are ubiquitously expressed in mammals with high levels found in the central nervous system (CNS) and in cancer. There are two subtypes of sigma receptors, sigma-1 and sigma-2. Although sigma-1 receptors promote cell growth and thus inhibit cell death, activation of sigma-2 receptors was reported to trigger cell death^[3]. Siramesine hydrochloride is a selective sigma receptors agonist with IC₅₀s of 17 and 0.12 nM for sigma-1 and sigma-2 receptors, respectively^[4]. In all cell lines tested, the siramesine concentration found to induce significant cell death within 8 h was in the range of 20 -30 μM, whereas 90% of cells were dead after treatment with 40–50 μM siramesine. Six hours post treatment with 25 or 40 μM siramesine, HaCaT cells exhibited characteristic apoptotic morphology with chromatin condensation and apoptotic body formation. In HaCaT cells, significant accumulation of the proforms of cysteine cathepsin L and cathepsins B and C was observed upon treatment with siramesine concentrations ≤15 μM^[3].