S83816 |
SA4503 (dihydrochloride) |
源叶(MedMol) | 98% |
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- 产品描述: Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
- 靶点: IC50: 17.4 nM (σ1receptor, guinea pig brain membranes);Sigmareceptor
- 体外研究:
The sigma receptor might be involved in several diseases in the central nervous system. Cutamesine, 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. Cutamesine is 14-fold selective for σ1 (Ki=4.6 nM) over σ2 (Ki=63.1 nM) sites in guinea pig brain homogenates. Cutamesine 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. Cutamesine reduces the activation of the MAPK/ERK pathway and down-regulated the ionotropic glutamate receptor, GluR1
- 体内研究:
Cutamesine extends the survival time in the SOD1G93A mice
- 参考文献:
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.
- 溶解性: Soluble in DMSO、H2O
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.265 ml 11.327 ml 22.653 ml 5 mM 0.453 ml 2.265 ml 4.531 ml 10 mM 0.227 ml 1.133 ml 2.265 ml 50 mM 0.045 ml 0.227 ml 0.453 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)