Nebentan potassium

尼苯坦钾

Nebentan potassium

N654865-1ml

1ml

10mM in DMSO

干燥,-80℃储存

超低温冰袋运输

Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ET A receptor antagonist through the modification of Bosentan . Nebentan potassium inhibits [ 125 I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with K i of 0.697 nM and 569 nM, respectively YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo . In Vitro Nebentan potassium inhibits the specific binding of [ 125 I] endothelin-1 to endothelin ET A and ET B receptors in a concentration dependent manner, K i 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 ET B receptors, with K i values of 569 nM and 155 nM,respectively. In measurement of intracellular Ca 2+ concentration, Nebentan potassium concentration-dependently inhibits the increase in [Ca 2+ ]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC 50 values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:ET A 0.679 nM (Ki) ET B 569 nM (Ki)

Nebentan 钾（YM598）是一种通过对 Bosentan ( HY-A0013 ) 进行修饰的强效、选择性和口服活性非肽内皮素 ET A 受体拮抗剂。Nebentan 钾可抑制[125 I]内皮素-1 与克隆人内皮素 ETA 的结合。

342005-82-7(DMSO)

C24H20KN5O5S

529.61 g/mol

COC1=CC=CC=C1OC2=C(N=C(N=C2OC)C3=NC=CC=N3)[N-]S(=O)(=O)C=CC4=CC=CC=C4.[K+]