Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 37.00 | |
5 mg | In stock | $ 57.00 | |
10 mg | In stock | $ 102.00 | |
25 mg | In stock | $ 235.00 | |
50 mg | In stock | $ 450.00 | |
100 mg | In stock | $ 663.00 | |
500 mg | In stock | $ 1,390.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 117.00 |
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. |
Targets&IC50 | σ1:17.4 nM |
In vitro | The sigma receptor might be involved in several diseases in the central nervous system. SA4503, a potent σ1receptor agonist, has 103-fold higher affinity for σ1 (IC50=17.4 nM) than σ2 (IC50=1,784 nM) sites in guinea pig brain membranes. SA4503 is 14-fold selective for σ1 (Ki=4.6 nM) over σ2 (Ki=63.1 nM) sites in guinea pig brain homogenates[1]. SA4503 protects motor neuron NSC34 cells against superoxide dismutase 1 and serum free neurotoxicity. It upregulates the phosphorylation levels of Akt and extracellular signal-regulated kinase (ERK) 1/2[2]. SA4503 reduces the activation of the MAPK/ERK pathway and down-regulated the ionotropic glutamate receptor, GluR1[3]. |
In vivo | SA4503 extends the survival time in the SOD1 g93A mice[2]. |
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]. |
Synonyms | AGY94806 dihydrochloride, SA4503 (dihydrochloride), SA4503 dihydrochloride |
Molecular Weight | 441.43 |
Formula | C23H32N2O2·2HCl |
CAS No. | 165377-44-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (67.96 mM), sonification/heating is recommended.
You can also refer to dose conversion for different animals. More
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Cutamesine dihydrochloride 165377-44-6 GPCR/G Protein Sigma receptor Sigma Receptor AGY 94806 Dihydrochloride AGY94806 dihydrochloride SA-4503 Dihydrochloride SA 4503 Cutamesine Dihydrochloride AGY94806 AGY 94806 AGY94806 Dihydrochloride AGY-94806 Dihydrochloride inhibit Inhibitor SA4503 SA4503 Dihydrochloride SA 4503 Dihydrochloride AGY-94806 SA-4503 SA4503 (dihydrochloride) SA4503 dihydrochloride Cutamesine inhibitor