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Siramesine (Lu 28-179) 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) 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 5,970 | 1-2周 | |
50 mg | ¥ 7,918 | 1-2周 |
产品描述 | Siramesine (Lu 28-179)(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 |
体内活性 | SA4503或siramesine与MEM(以及AMA)联合给药,可减少大鼠的不动时间。SA4503和AMA共同给药的效果被孕酮(一种sigma1受体拮抗性神经甾体)所拮抗。 |
别名 | 西拉美新, Lu 28-179 |
分子量 | 454.58 |
分子式 | C30H31FN2O |
CAS No. | 147817-50-3 |
Smiles | C(CCCC=1C=2C(N(C1)C3=CC=C(F)C=C3)=CC=CC2)N4CCC5(C=6C(CO5)=CC=CC6)CC4 |
密度 | 1.19 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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