siramesine
Modify Date: 2024-01-09 17:03:09
siramesine structure
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Common Name | siramesine | ||
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| CAS Number | 147817-50-3 | Molecular Weight | 454.578 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 611.4±55.0 °C at 760 mmHg | |
| Molecular Formula | C30H31FN2O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 323.6±31.5 °C | |
Use of siramesineSiramesine(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. IC50 value:Target: sigma-2 receptor; lysosome-destabilizing agentsiramesine 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] |
| Name | 1'-[4-[1-(4-fluorophenyl)indol-3-yl]butyl]spiro[1H-2-benzofuran-3,4'-piperidine] |
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| Synonym | More Synonyms |
| Description | 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. IC50 value:Target: sigma-2 receptor; lysosome-destabilizing agentsiramesine 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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| Related Catalog | |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 611.4±55.0 °C at 760 mmHg |
| Molecular Formula | C30H31FN2O |
| Molecular Weight | 454.578 |
| Flash Point | 323.6±31.5 °C |
| Exact Mass | 454.242035 |
| PSA | 17.40000 |
| LogP | 9.19 |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Index of Refraction | 1.629 |
| Storage condition | -20℃ |
| Hazard Codes | Xi |
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siramesine CAS#:147817-50-3 |
| Literature: Journal of Medicinal Chemistry, , vol. 38, # 11 p. 1998 - 2008 |
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siramesine CAS#:147817-50-3 |
| Literature: Journal of Labelled Compounds and Radiopharmaceuticals, , vol. 48, # 1 p. 31 - 43 |
|
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siramesine CAS#:147817-50-3 |
| Literature: Journal of Labelled Compounds and Radiopharmaceuticals, , vol. 48, # 1 p. 31 - 43 |
|
~%
siramesine CAS#:147817-50-3 |
| Literature: Journal of Medicinal Chemistry, , vol. 38, # 11 p. 1998 - 2008 |
|
~%
siramesine CAS#:147817-50-3 |
| Literature: Journal of Medicinal Chemistry, , vol. 38, # 11 p. 1998 - 2008 |
![3H-Spiro[2-benzofuran-1,4'-piperidine] structure](https://www.chemsrc.com/caspic/450/38309-60-3.png)
| QCR-66 |
| UNII-3IX8CWR24V |
| 1'-{4-[1-(4-Fluorophenyl)-1H-indol-3-yl]butyl}-3H-spiro[2-benzofuran-1,4'-piperidine] |
| siramesine |
| Lu 28-179 |
| Spiro[isobenzofuran-1(3H),4'-piperidine], 1'-[4-[1-(4-fluorophenyl)-1H-indol-3-yl]butyl]- |