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Siramesine | Selective sigma-2 agonist

Siramesine (Lu 28-179, 147817-50-3) is a σ2 selective agonist (IC50’s: σ1 = 17nM, σ2 = 0.2nM).1 It produced non-sedating potent and long-last anxiolytic effects in rodents.2 Siramesine induced caspase-independent programmed cell death in various cancer cell lines via increased levels of ROS and lysosomal leakage.3,4,5 Mitochondrial destabilization via loss of membrane potential and increased ROS has also been offered as a mechanism of action for the triggering of cell death by Siramesine.6

 

References/Citations

1) Perregaard et al. (1995), Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles; J. Med. Chem. 38 1998
2) Sanchez et al. (1997), The selective sigma2-ligand Lu 280179 has potent anxiolytic effects in rodents; J. Pharmacol. Exp. Ther. 283 1323
3) Ostenfeld et al. (2005), Effective tumor cell death by sigma-2 receptor ligand siramesine involves lysosomal leakage and oxidative stress; Cancer Res. 65 8975
4) Ostenfeld et al. (2008), Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation; Autophagy 4 487
5) Dielschneider et al. (2016), Lysosomotropic agents selectively target chronic lymphocytic leukemia cells due to altered sphingolipid metabolism; Leukemia 30 1290
6) Cesen et al. (2013), Siramesine triggers cell death through destabilization of mitochondria, but not lysosomes; Cell Death Dis. 4 e818

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Catalog#  10-4202-0005

$70.00
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CAS:
147817-50-3
Catalog Number:
10-4202
Activity:
Selective sigma-2 agonist
Chemical Name:
1’-[4-[1-(4-Fluorophenyl)indol-3-yl]butyl]spiro[1H-2-benzofuran-3,4’-piperidine;
Alternate Names:
Lu 28-179
Molecular Weight:
454.59
Molecular Formula:
C30H31FN2O
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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