1. GPCR/G Protein
    Neuronal Signaling
  2. Sigma Receptor
  3. Siramesine

Siramesine (Synonyms: Lu 28-179)

Cat. No.: HY-14221
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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.

For research use only. We do not sell to patients.

Siramesine Chemical Structure

Siramesine Chemical Structure

CAS No. : 147817-50-3

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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].

In Vitro

Siramesine 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 (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 (0-40 μM; 2-48 hours) activates caspases in HaCaT and in U-87MG cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

454.58

Formula

C₃₀H₃₁FN₂O

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Siramesine
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