| Name | Cutamesine dihydrochloride |
| Description | Cutamesine dihydrochloride (SA4503 dihydrochloride) is a selective σ1 receptor agonist (IC50: 17.4 nM). It shows selectivity for σ1 over σ2 receptors, and inhibits angiotensin II-induced cardiomyocyte hypertrophy in vitro and attenuates myocardial hypertrophy in vivo. In a rat model of experimental stroke, it enhances brain plasticity and sensorimotor function. |
| Cell Research | The NSC34 cells are seeded at a density of 7000 cells per well into 96-well plates with D-MEM and transfected using Lipofectamine 2000 mixed with 2 μg /mL of plasmid vector in D-MEM for 6 h. After 6 h, the cell-culture medium is replaced with fresh D-MEM and culture and allowed to proceed for a further 42 h. The cells are then transferred to serum-free D-MEM and immediately treated with SA4503 at a final concentration of 1, 3, or 10 nM[2]. |
| In vitro | The sigma receptor is implicated in various central nervous system diseases. SA4503, a potent σ1 receptor agonist, exhibits a 103-fold higher affinity for σ1 (IC50=17.4 nM) than σ2 (IC50=1,784 nM) in guinea pig brain membranes and is 14-fold selective for σ1 (Ki=4.6 nM) over σ2 (Ki=63.1 nM) in guinea pig brain homogenates[1]. SA4503 protects motor neuron NSC34 cells against superoxide dismutase 1 and serum-free neurotoxicity, upregulating phosphorylation levels of Akt and extracellular signal-regulated kinase (ERK) 1/2[2], while reducing MAPK/ERK pathway activation and down-regulating the ionotropic glutamate receptor, GluR1[3]. |
| In vivo | SA4503 extends the survival time in the SOD1 g93A mice[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.27 mM), Sonication is recommended.
DMSO : 10 mg/mL (22.65 mM), Sonication and heating are recommended.
H2O : 100 mg/mL (226.54 mM), Sonication is recommended.
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| Keywords | σ1 | Sigmareceptor | Sigma Receptor | SA-4503 Dihydrochloride | SA4503 Dihydrochloride | SA-4503 | SA4503 | SA 4503 Dihydrochloride | SA 4503 | Inhibitor | inhibit | Cutamesine Dihydrochloride | Cutamesine | AGY-94806 Dihydrochloride | AGY94806 Dihydrochloride | AGY-94806 | AGY94806 | AGY 94806 Dihydrochloride | AGY 94806 |
| Inhibitors Related | Amitriptyline | Opipramol | L-693,403 maleate | Noscapine | Oxeladin citrate | Amitriptyline hydrochloride | S1R agonist 2 | 4-PPBP maleate | Glycerol phenylbutyrate | Sigma-1 receptor antagonist 1 | KSK67 | AB21 HCl |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Obesity Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library |
United States
