Min.Order / FOB Price:Get Latest Price
100 Gram |
FOB Price: USD 1.0000 |
Siramesine hydrochloride, Lu-28-179 SiraMesine, Lu-28-179;SiraMesine (hydrochloride);1'-[4-[1-(4-Fluorophenyl)-1H-indol-3-yl]butyl]spiro[isobenzofuran-1(3H),4'-piperidine] monohydrochloride;Siramesine (HCl salt), Lu-28-179;Siramesine hy 224177-60-0
Siramesine(Lu 28-179) Hcl 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.
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]
About|Contact|Cas|Product Name|Molecular|Country|Encyclopedia
Message|New Cas|MSDS|Service|Advertisement|CAS DataBase|Article Data|Manufacturers | Chemical Catalog
©2008 LookChem.com,License: ICP
NO.:Zhejiang16009103
complaints:service@lookchem.com Desktop View