Siramesine Hydrochloride

Cat. No. IC23159

CAS. No. 224177-60-0

Key Features and Details

Category

Inhibitor&Activator

Purity

99.74%

Formula

C30H32ClFN2O

Product Size

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Product Details

Product Name

Siramesine Hydrochloride

CAS No.

224177-60-0

Molecular Weight

491.04

Synonyms

Lu 28-179 hydrochloride

Formula

C30H32ClFN2O

Appearance

Solid

Purity

99.74%

SMILES

FC1=CC=C(N2C=C(CCCCN3CCC4(CC3)OCC5=C4C=CC=C5)C6=C2C=CC=C6)C=C1.Cl

Product Overview

Description

Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride 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 hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity.

In Vitro Activity

Siramesine hydrochloride 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. Siramesine (0-50μM; 8 hours) hydrochloride 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). Siramesine (0-40 μM; 2-48 hours) hydrochloride activates caspases in HaCaT and in U-87MG cells.

Storage & Handling

Storage

4 °C, sealed storage, away from moisture In solvent : -80 °C, 6 months; -20 °C, 1 month (sealed storage, away from moisture)

Shipping

Room temperature in continental US; may vary elsewhere.

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