Nebentan 钾盐 T36008

Product Introduction
Bioactivity


英文名: Nebentan potassium

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].

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 125 mg/mL (236.02 mM)


关键字: Nebentan potassium

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