Siramesine fumarate
Based on 6 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 163630-79-3
- Formula: C34H35FN2O5
- Molecular Weight:570.65
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Siramesine fumarate
MoreAll Sigma Receptor Isoforms
More
Biological Activity
Siramesine fumarate displays the binding affinities: IC50 (sigma 1)=17 nM, IC50 (sigma 2)=0.12 nM, IC50 (5-HT1A)=21000 nM, IC50 (5-HT1A)=2000 nM, IC50 (D2)=800 nM, IC50 (alpha 1)=330 nM[1].
Siramesine fumarate (0-50μM; 8 hours) induces cell death in various cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y and glioblastoma cell line U-87MG)[2].
Siramesine fumarate (0-40 μM; 2-48 hours) activates caspases in HaCaT and in U-87MG cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 163630-79-3
-
Molecular Weight 570.65
-
Formula C34H35FN2O5
-
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
-
Synonyms
LU-28-179 fumarate
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
-
Journal Impact Factor
-
Most Recent
-
J Am Chem Soc
Fluorinated Ribonucleocarbohydrate Nanoparticles Allow Ultraefficient mRNA Delivery and Protein Expression in Tumor-Associated Myeloid Cells. [Abstract]2025 Mar 26. PMID: 40135499 -
Adv Sci (Weinh)
2023 May;10(13):e2300311. PMID: 36905240 -
Sci Adv
Quantitative prediction of siRNA complexation by ionizable drugs enables their codelivery in nanoparticles. [Abstract]2026 Jun 12;12(24):eaed2731. PMID: 42284421 -
J Pharmacol Exp Ther
Characterization of CM572, a Selective Irreversible Partial Agonist of the Sigma-2 Receptor with Antitumor Activity. [Abstract]2015 Aug;354(2):203-12. PMID: 26034081 -
-
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
[3]. Ostenfeld MS, et al. Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Autophagy. 2008;4(4):487-499. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Siramesine fumarate Related Classifications
HY-14221B Related Classifications
Powered by Bioz