Siramesine, Lu-28-179

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100 Gram	FOB Price: USD 1.0000

100 Gram

FOB Price: USD 1.0000

Min.Order :100 Gram
Purity: 98%
Payment Terms : L/C

Keywords

Siramesine, Lu-28-179 SIRAMESINE;1'-(4-(1-(4-fluorophenyl)-1H-indol-3-yl)butyl)-3H-spiro[isobenzofuran-1,4'-piperidine] 147817-50-3

Quick Details

Appearance:white powder
Application:CAS：147817-50-3；
PackAge:100g,500g,1kg,25kg/drum
ProductionCapacity:1000|Gram|Week
Storage:Dry seal
Transportation:shipping

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Details:

Siramesine, a sigma-2 receptor agonist siramesine has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.
IC50 value:
Target: sigma-2 receptor; 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 [1]. Siramesine, a sigma-2 receptor agonist originally developed as an anti-depressant, can induce cell death in transformed cells through a mechanism involving lysosomal destabilization [2].
in vivo: 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. Combined treatment with siramesine and AMA was modified by neither progesterone nor BD1047 (a novel sigma antagonist with preferential affinity for sigma1 sites) [3]

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