Biological Activity
Selective σ1 receptor agonist (IC50 = 17.4 nM). Exhibits selectivity for σ1 over σ2 receptors. Inhibits angiotensin II-induced cardiomyocyte hypertrophy in vitro and attenuates myocardial hypertrophy in vivo. Enhances brain plasticity and sensorimotor function in a rat model of experimental stroke.
Compound Libraries
SA 4503 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 441.43 |
| Formula | C23H32N2O2.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 165377-44-6 |
| PubChem ID | 9954941 |
| InChI Key | XWOXAKBQEMQMFH-UHFFFAOYSA-N |
| Smiles | COC1=C(OC)C=CC(CCN2CCN(CCCC3=CC=CC=C3)CC2)=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.83 | 20 | |
| water | 44.14 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 441.43. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.27 mL | 11.33 mL | 22.65 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.53 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.27 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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References
References are publications that support the products' biological activity.
Ruscher et al (2011) The sigma-1 receptor enhances brain plasticity and functional recovery after experimental stroke. Brain 134 732 PMID: 21278085
Matsuno et al (1996) Binding properties of SA4503, a novel and selective sigma 1 receptor agonist. Eur.J.Pharmacol. 306 271 PMID: 8813641
Tagashira et al (2013) Stimulation of s1-receptor restores abnormal mitochondrial Ca2+ mobilization and ATP production following cardiac hypertrophy. Biochim.Biophys.Acta 1830 3082 PMID: 23298811
Lever et al (2006) σ1 and σ2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse 59 350 PMID: 16463398
Keywords: SA 4503 dihydrochloride, supplier, SA4503, dihydrochloride, selective, agonists, sigma1, receptor, σ1, Sigma1, Receptors, Sigma1, Receptors, Tocris Bioscience
