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Siramesine HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Siramesine HCl图片
CAS NO:224177-60-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 491.05
Formula C30H32ClFN2O
CAS No.224177-60-0 (HCl);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>10 mM
Water: <1 mg/mL
Ethanol: NA
SMILES CodeFC1=CC=C(N2C=C(CCCCN3CCC4(CC3)OCC5=CC=CC=C45)C6=C2C=CC=C6)C=C1.[H]Cl
SynonymsLu-28-179; Lu 28179; Lu 28-179; Lu-28179; Lu28-179; Lu28179; Siramesine HCl; Siramesine hydrochloride;
实验参考方法
In Vitro

In vitro activity: Formerly known as Lu-28-179, siramesine is a potent and selective agonist of sigma-2 receptor agonist. Siramesine is able to trigger cancer cell death through destabilisation of mitochondria and exhibit promising anticancer activity in vivo. 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.


Cell Assay: iramesine 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. In contrast to the rapid loss of MMP above 20 μM siramesine, a rapid increase in lysosomal pH was observed at all concentrations tested (5-40 μM); however, it was not accompanied by lysosomal membrane permeabilisation (LMP) and the release of lysosomal enzymes into the cytosol. Increased lysosomal pH reduced the lysosomal degradation potential as indicated by the accumulation of immature forms of cysteine cathepsins. The lipophilic antioxidant α-tocopherol, but not the hydrophilic antioxidant N-acetyl-cysteine, considerably reduced cell death and destabilisation of mitochondrial membranes, but did not prevent the increase in lysosomal pH. At concentrations below 15 μM, siramesine triggered cell death after 2 days or later, which seems to be associated with a general metabolic and energy imbalance due to defects in the endocytic pathway, intracellular trafficking and energy production, and not by a specific molecular event.

In VivoSA4503 or siramesine given jointly with MEM (as well as with AMA) decreased the immobility time in rats.
Animal modelRats
Formulation & DosageNA
References Cell Death Dis. 2013 Oct 3;4:e818; The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats. J Physiol Pharmacol. 2006 Jun;57(2):217-29.