Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Cutamesine dihydrochloride (SA4503 dihydrochloride) 是一种选择性 σ1 受体激动剂,IC50值为 17.4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 268 | 现货 | ||
2 mg | ¥ 378 | 现货 | ||
5 mg | ¥ 613 | 现货 | ||
10 mg | ¥ 988 | 现货 | ||
25 mg | ¥ 1,670 | 现货 | ||
50 mg | ¥ 2,480 | 现货 | ||
100 mg | ¥ 3,690 | 现货 | ||
500 mg | ¥ 8,250 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 712 | 现货 |
产品描述 | 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. |
靶点活性 | σ1:17.4 nM |
体外活性 | 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]. |
体内活性 | SA4503 extends the survival time in the SOD1 g93A mice[2]. |
细胞实验 | 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]. |
别名 | AGY94806 dihydrochloride, 库他美新二盐酸盐, SA4503 (dihydrochloride), SA4503 dihydrochloride |
分子量 | 441.43 |
分子式 | 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), Sonication and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2654 mL | 11.3268 mL | 22.6536 mL | 56.6341 mL |
5 mM | 0.4531 mL | 2.2654 mL | 4.5307 mL | 11.3268 mL | |
10 mM | 0.2265 mL | 1.1327 mL | 2.2654 mL | 5.6634 mL | |
20 mM | 0.1133 mL | 0.5663 mL | 1.1327 mL | 2.8317 mL | |
50 mM | 0.0453 mL | 0.2265 mL | 0.4531 mL | 1.1327 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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 库他美新二盐酸盐 SA 4503 Dihydrochloride AGY-94806 SA-4503 SA4503 (dihydrochloride) SA4503 dihydrochloride Cutamesine inhibitor