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Product 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].
Web ID
– HY-14221B
Shipping
– Room temperature
Molecular Formula
– C34H35FN2O5
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.|[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.
CAS Number
– 163630-79-3
Molecular Weight
– 570.65
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
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Sigma Receptor
Pathway
– Neuronal Signaling
Product type
– Reference compound
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