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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[1][2][3].

Product Specifications

CAS Number

163630-79-3

Product Name Alternative

LU-28-179 (fumarate)

UNSPSC

12352005

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-fumarate.html

Solubility

10 mM in DMSO

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

Molecular Formula

C34H35FN2O5

Molecular Weight

570.65

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

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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