Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EMD638683 是一种具有抗高血压效力的新型 SGK 抑制剂,IC50=3 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 673 | 现货 | ||
5 mg | ¥ 1,290 | 现货 | ||
10 mg | ¥ 2,080 | 现货 | ||
25 mg | ¥ 3,860 | 现货 | ||
50 mg | ¥ 5,530 | 现货 | ||
100 mg | ¥ 7,750 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,430 | 现货 |
产品描述 | EMD638683,a novel SGK inhibitor with antihypertensive potency(with an IC50 of 3 μM). |
靶点活性 | SGK1:3 μM |
体外活性 | EMD638683 treatment significantly augmented the radiation-induced decrease of forward scatter, increase of phosphatidylserine exposure, decrease of mitochondrial potential, increase of caspase 3 activity, increase of DNA fragmentation and increase of late apoptosis. The in vivo development of tumors following chemical carcinogenesis was significantly blunted by treatment with EMD638683[1]. |
体内活性 | Within 24 hours in vivo EMD638683 treatment significantly decreased blood pressure in fructose/saline-treated mice but not in control animals or in SGK1 knockout mice.?EMD638683 failed to alter the blood pressure in SGK1 knockout mice.?Following chronic (4 weeks) fructose/high salt treatment, additional EMD638683 treatment again decreased blood pressure.?EMD638683 thus abrogates the salt sensitivity of blood pressure in hyperinsulinism without appreciably affecting blood pressure in the absence of hyperinsulinism.?EMD638683 tended to increase fluid intake and urinary excretion of Na(+), significantly increased urinary flow rate and significantly decreased body weight[2]. |
细胞实验 | Colon carcinoma (Caco-2) cells were exposed to EMD638683 with or without exposure to radiation (3 Gray) and cell volume was estimated from forward scatter, phosphatidylserine exposure from annexin V binding, mitochondrial potential from JC-9 fluorescence, caspase 3 activity from CaspGlow Fluorescein staining, DNA degradation from propidium iodide staining as well as late apoptosis from annexin-V FITC and propidium iodide double staining.?In vivo tumor growth was determined in wild type mice subjected to chemical carcinogenesis (intraperitoneal injection of 20 mg/kg 1,2-dimethylhydrazine followed by three cycles of 30 g/L synthetic dextran sulfate sodium in drinking water for 7 days)[1]. |
分子量 | 364.34 |
分子式 | C18H18F2N2O4 |
CAS No. | 1181770-72-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (137.23 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7447 mL | 13.7234 mL | 27.4469 mL | 68.6172 mL |
5 mM | 0.5489 mL | 2.7447 mL | 5.4894 mL | 13.7234 mL | |
10 mM | 0.2745 mL | 1.3723 mL | 2.7447 mL | 6.8617 mL | |
20 mM | 0.1372 mL | 0.6862 mL | 1.3723 mL | 3.4309 mL | |
50 mM | 0.0549 mL | 0.2745 mL | 0.5489 mL | 1.3723 mL | |
100 mM | 0.0274 mL | 0.1372 mL | 0.2745 mL | 0.6862 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。
EMD638683 1181770-72-8 Metabolism SGK inhibit Serum and glucocorticoid-regulated kinase Inhibitor Serum-glucocorticoid regulated kinase EMD 638683 EMD-638683 inhibitor