Siramesine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Siramesine(Lu 28-179) 是一种选择性 sigma-2 受体激动剂，已被证明可以触发癌细胞死亡并在体内表现出有效的抗癌活性。

Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.lysosome-destabilizing agent siramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. In HaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrial membrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptotic morphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMP was rapidly lost.

Siramesine displays the binding affinities: IC50 (sigma 1)=17 nM, IC50 (sigma 2)=0.12 nM, IC50 (5-HT1A)=21000 nM, IC50 (5-HT1A)=2000 nM, IC50 (D2)=800 nM, IC50 (alpha 1)=330 nM.Siramesine (0-50μM; 8 hours) induces cell death in various cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y and glioblastoma cell line U-87MG).Siramesine (0-40 μM; 2-48 hours) activates caspases in HaCaT and in U-87MG cells.

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Lu 28-179

Metabolic Enzyme/Protease

PPAR

sigma-2 receptor

Cancer

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147817-50-3

454.58

C30H31FN2O

>98% (HPLC)

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C1CN(CCC12C3=CC=CC=C3CO2)CCCCC4=CN(C5=CC=CC=C54)C6=CC=C(C=C6)F

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(-20℃)

With Ice Pack

≥ 2 years