Siramesine,163630-79-3

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Siramesine fumarate

CAS No. : 163630-79-3

MCE 国际站：Siramesine fumarate

产品活性：Siramesine (Lu 28-179) fumarate 是一种有效的 sigma-2 受体激动剂。Siramesine fumarate 对 sigma-2 受体具有亚纳摩尔亲和力 (IC₅₀=0.12?nM)，并且对 sigma-2 受体的选择性是 sigma-1 受体的 140倍 (IC₅₀=17?nM)。Siramesine fumarate 通过线粒体的不稳定而不是溶酶体触发细胞死亡。Siramesine fumarate 显示出强大的抗癌活性。

研究领域：Neuronal Signaling

作用靶点：Sigma Receptor

In Vitro: Siramesine fumarate displays the binding affinities: IC₅₀ (sigma 1)=17 nM, IC₅₀ (sigma 2)=0.12 nM, IC₅₀ (5-HT_1A)=21000 nM, IC₅₀ (5-HT_1A)=2000 nM, IC₅₀ (D₂)=800 nM, IC₅₀ (alpha 1)=330 nM.
Siramesine fumarate (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 fumarate (0-40 μM; 2-48 hours) activates caspases in HaCaT and in U-87MG cells.

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