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Product Description
– Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine 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 triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity[1][2][3].
Web ID
– HY-14221
Shipping
– Room temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C30H31FN2O
Citations
– Adv Sci (Weinh). 2023 Mar 11;e2300311.|Dean Francis. 2023 Jun.|J Pharmacol Exp Ther. 2015 Aug;354(2):203-12. |Patent. US20220305013A1.
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
– 147817-50-3
Molecular Weight
– 454.58
SMILES
– FC1=CC=C(N2C=C(CCCCN3CCC4(CC3)OCC5=C4C=CC=C5)C6=C2C=CC=C6)C=C1
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Sigma Receptor
Isoform
– Sigma 1 Receptor
Pathway
– Neuronal Signaling
Product type
– Reference compound
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