Siramesine 是sigma-2受体激动剂，通过线粒体的不稳定溶酶体触发细胞死亡，有强大的抗癌活性。它对 sigma-2 受体具有亚纳摩尔亲和力，IC50为 0.12?nM。它对 sigma-2 受体的选择性是 sigma-1 受体的 140倍，IC50为 17?nM。

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

SA4503 or siramesine given jointly with MEM (as well as with AMA) decreased the immobility time in rats. The effect of SA4503 and AMA co-administration was antagonized by progesterone, a sigma1 receptor antagonistic neurosteroid.

147817-50-3

C30H31FN2O

454.589

西拉美新;Lu 28-179

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years