163630-79-3
Chemical Structure
Siramesine fumarate
Synonym(s): LU-28-179 fumarate
- CAS No.: 163630-79-3
- Formula:C34H35FN2O5
- Molecular Weight:570.65
IUPAC Name: 1'-(4-(1-(4-fluorophenyl)-1H-indol-3-yl)butyl)-3H-spiro[isobenzofuran-1,4'-piperidine] fumarate
InChIKey: VONJQLKJOYOVBE-WLHGVMLRSA-N
SMILES: FC1=CC=C(C=C1)N2C=C(C3=C2C=CC=C3)CCCCN4CCC5(OCC6=C5C=CC=C6)CC4.O=C(/C=C/C(O)=O)O
Biological Activity: 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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Siramesine fumarate | 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. | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [3]. Ostenfeld MS, et al. Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Autophagy. 2008;4(4):487-499. [Content Brief]
