Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan potassium inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 763 | 现货 | ||
5 mg | ¥ 1,880 | 现货 | ||
10 mg | ¥ 2,790 | 现货 | ||
25 mg | ¥ 4,670 | 现货 | ||
50 mg | ¥ 6,660 | 现货 | ||
100 mg | ¥ 8,880 | 现货 | ||
500 mg | ¥ 17,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,390 | 现货 |
产品描述 | Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan potassium inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. |
靶点活性 | ETB:569 nM (Ki), ETA:0.679 nM (Ki) |
体外活性 | Nebentan potassium inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dependent manner, Ki values are 0.697 nM and 1.53 nM for human and rat endothelin ETA receptors, respectively. In contrast, YM598 exhibits low affinities for human and rat endothelin ETB receptors, with Ki values of 569 nM and 155 nM,respectively[1].In measurement of intracellular Ca2+ concentration, Nebentan potassium concentration-dependently inhibits the increase in [Ca2+]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC50 values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively[1]. |
体内活性 | Nebentan potassium (oral administration; 0.1-1 mg/kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy[2].Nebentan potassium (oral administration; 1 mg/kg; 30 weeks) significantly ameliorates the poor survival rate of CHF rats, it markedly reduces the hypertrophy of both ventricles as well as pulmonary congestion[2]. |
分子量 | 530.62 |
分子式 | C24H21KN5O5S |
CAS No. | 342005-82-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (236.02 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8846 mL | 9.4229 mL | 18.8459 mL | 47.1147 mL |
5 mM | 0.3769 mL | 1.8846 mL | 3.7692 mL | 9.4229 mL | |
10 mM | 0.1885 mL | 0.9423 mL | 1.8846 mL | 4.7115 mL | |
20 mM | 0.0942 mL | 0.4711 mL | 0.9423 mL | 2.3557 mL | |
50 mM | 0.0377 mL | 0.1885 mL | 0.3769 mL | 0.9423 mL | |
100 mM | 0.0188 mL | 0.0942 mL | 0.1885 mL | 0.4711 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。
Nebentan potassium 342005-82-7 Inhibitor inhibitor inhibit