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Siramesine

CAT: 0804-HY-14221-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-14221-01Size:5 mg
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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].
CAS Number
147817-50-3
Product Name Alternative
Lu 28-179
UNSPSC
12352005
Hazard Statement
H315, H319
Target
Sigma Receptor
Type
Reference compound
Related Pathways
Neuronal Signaling
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/siramesine.html
Purity
98.98
Solubility
10 mM in DMSO
Smiles
FC1=CC=C(N2C=C(CCCCN3CCC4(CC3)OCC5=C4C=CC=C5)C6=C2C=CC=C6)C=C1
Molecular Formula
C30H31FN2O
Molecular Weight
454.58
Precautions
H315, H319
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Sigma 1 Receptor
Citation 01
Adv Sci (Weinh) . 2023 May;10 (13) :e2300311.|Dean Francis. 2023 Jun.|J Pharmacol Exp Ther. 2015 Aug;354 (2) :203-12. |J Am Chem Soc. 2025 Apr 9;147 (14) :11766-11776.|Patent. US20220305013A1.

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