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Purity: ≥98%
SA4503 dihydrochloride (also known as AGY94806 dihydrochloride and Cutamesine dihydrochloride), is a potent sigma-1 (σ1) receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. It is under development for recovery enhancement after acute ischemic stroke. 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. SA-4503 protects against retinal cell death in vitro and in vivo by the agonistic effect of σ1 receptor. Therefore, σ1 receptor may serve as a potential therapeutic target in retinal diseases mediated by photoreceptor degeneration.
| ln Vitro |
The central nervous system is home to a number of disorders that may be related to the sigma receptor. In guinea pig brain membranes, cutamesine, a strong σ1receptor agonist, has a 103-fold greater affinity for σ1 (IC50=17.4 nM) sites than σ2 (IC50=1,784 nM). In guinea pig brain homogenates, cutamesine is 14-fold more selective for σ1 (Ki=4.6 nM) sites than σ2 (Ki=63.1 nM)[1]. Cutamesine shields motor neuron NSC34 cells from serum free neurotoxicity and superoxide dismutase 1. Extracellular signal-regulated kinase (ERK) 1/2 and Akt are both phosphorylated more highly by it[2]. Cutamesine downregulates the ionotropic glutamate receptor, GluR1, and lessens the activation of the MAPK/ERK pathway[3].
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| ln Vivo |
In SOD1G93A mice, cutamesine prolongs their survival period[2].
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| References |
[1]. Lever JR, et al. Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse. 2006 May;59(6):350-8.
[2]. Tuerxun T, et al. SA4503, a sigma-1 receptor agonist, prevents cultured cortical neurons from oxidative stress-induced cell death via suppression of MAPK pathway activation and glutamate receptor expression. Neurosci Lett. 2010 Jan 29;469(3):303-8 |
| Molecular Formula |
C₂₃H₃₄CL₂N₂O₂
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| Molecular Weight |
441.43
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| CAS # |
165377-44-6
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| Related CAS # |
Cutamesine;165377-43-5
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| SMILES |
COC1=CC=C(C=C1OC)CCN2CCN(CCCC3=CC=CC=C3)CC2.[H]Cl.[H]Cl
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 33.33 mg/mL (75.50 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2654 mL | 11.3268 mL | 22.6536 mL | |
| 5 mM | 0.4531 mL | 2.2654 mL | 4.5307 mL | |
| 10 mM | 0.2265 mL | 1.1327 mL | 2.2654 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Neurosci Lett.2010 Jan 29;469(3):303-8. |
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 Neurosci Lett.2010 Jan 29;469(3):303-8. |
 Neurosci Lett.2010 Jan 29;469(3):303-8. |
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