Siramesine fumarate salt
Modify Date: 2024-01-30 11:41:34
Siramesine fumarate salt structure
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Common Name | Siramesine fumarate salt | ||
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| CAS Number | 163630-79-3 | Molecular Weight | 570.65 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C34H35FN2O5 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
Use of Siramesine fumarate saltSiramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity[1][2][3]. |
| Name | 1'-{4-[1-(4-Fluorophenyl)-1H-indol-3-yl]butyl}-3H-spiro[2-benzofuran-1,4'-piperidine] (2E)-2-butenedioate (1:1) |
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| Synonym | More Synonyms |
| Description | Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity[1][2][3]. |
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| Related Catalog | |
| In Vitro | Siramesine fumarate displays the binding affinities: IC50 (sigma 1)=17 nM, IC50 (sigma 2)=0.12 nM, IC50 (5-HT1A)=21000 nM, IC50 (5-HT1A)=2000 nM, IC50 (D2)=800 nM, IC50 (alpha 1)=330 nM[1]. Siramesine fumarate (0-50μM; 8 hours) induces cell death in various cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y and glioblastoma cell line U-87MG)[2]. Siramesine fumarate (0-40 μM; 2-48 hours) activates caspases in HaCaT and in U-87MG cells[2]. |
| References |
| Molecular Formula | C34H35FN2O5 |
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| Molecular Weight | 570.65 |
| Exact Mass | 570.252991 |
| Storage condition | 2-8°C |
| RIDADR | NONH for all modes of transport |
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| 1'-{4-[1-(4-Fluorophenyl)-1H-indol-3-yl]butyl}-3H-spiro[2-benzofuran-1,4'-piperidine] (2E)-2-butenedioate (1:1) |
| Spiro[isobenzofuran-1(3H),4'-piperidine], 1'-[4-[1-(4-fluorophenyl)-1H-indol-3-yl]butyl]-, (2E)-2-butenedioate (1:1) |
| MFCD28016590 |