| Bioactivity | 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]. |
| Invitro | 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]. 0 --> Siramesine fumarate 相关抗体: |
| Name | Siramesine fumarate |
| CAS | 163630-79-3 |
| Formula | C34H35FN2O5 |
| Molar Mass | 570.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Perregaard J, et al. Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. J Med Chem. 1995;38(11):1998-2008. [2]. Česen MH, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013;4(10):e818. Published 2013 Oct 3. [3]. Ostenfeld MS, et al. Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Autophagy. 2008;4(4):487-499. |
Siramesine fumarate
CAS: 163630-79-3 F: C34H35FN2O5 W: 570.65
Siramesine(Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesinefumarate has a subnanomolar affinity for
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