store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dicirenone (SC26304) 对盐皮质激素受体 (MR)有抑制作用,对醛固酮对尿 K+:Na+ 比例的调节和 醛固酮与肾细胞质和核受体结合有抑制作用。
产品描述 | Dicirenone (SC26304) inhibits the Mineralocorticoid receptor (MR), aldosterone regulation of the urinary K+:Na+ ratio, and aldosterone binding to renal cytoplasmic and nuclear receptors. |
体内活性 |
In glycerol density gradients, cytoplasmic [3H]Aldosterone receptor complexes sediment at 8.5 S and 4 S in low concentrations of salt and at 4.5 S in high concentrations of salt. Similarly, cytoplasmic [3H]Dicirenone receptor complexes sediment at 3 S in low concentrations of salt and 4 S in high concentrations of salt. The cytoplasmic binding of [3H]Aldosterone and [3H]Dicirenone is similar in magnitude and involves the same set of sites. Under three sets of conditions - (i) in the intact rat, (ii) in kidney slices, and (iii) in reconstitution studies (mixing prelabeled cytoplasm with either purified renal nuclei or chromatin) - [3H]Dicirenone does not yield specific nuclear complexes, in contrast to the reproducible generation of these complexes with [3H]Aldosterone. Administration of Dicirenone (SC-26304) alone in doses of 3-600 μg/100 g of body weight has no effect on urinary Na+:creatinine or K+:creatinine ratios, expressed as urinary K+:Na+ ratios. Aldosterone (0.3 μg/100 g of body weight) increases the K+:Na+ ratio 5-fold. This increase is significantly inhibited by 180 μg/100 g of body weight of Dicirenone and completely inhibited by 600 μg/100 g of body weight. To correlate inhibitory action and receptor occupancy, the same doses of Dicirenone are given to rats injected with 0.036 μg of [3H]Aldosterone. A dose of 180 μg/100 g of body weight reduces specific binding of Aldosterone in cytoplasmic and nuclear fractions to less than half of the control levels, and 600 μg/100 g of body weight eliminates specific binding. The dose of Aldosterone used in the physiological studies is about eight times that used in the binding studies, but both doses are well below saturating amounts[1]. |
别名 | SC26304 |
分子量 | 428.56 |
分子式 | C26H36O5 |
CAS No. | 41020-79-5 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
Dicirenone 41020-79-5 Endocrinology/Hormones Membrane transporter/Ion channel ATPase Glucocorticoid Receptor SC26304 SC 26304 SC-26304 Inhibitor inhibitor inhibit