403604-85-3
403604-85-3 結構式
基本信息
Nebentan free base
Ethenesulfonamide, N-[6-methoxy-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]-2-phenyl-, (1E)-
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2024/01/25 | HY-106994 | Nebentan | 403604-85-3 | 5mg | 2500元 |
| 2024/01/25 | HY-106994 | Nebentan | 403604-85-3 | 10mM * 1mLin DMSO | 2700元 |
| 2024/01/25 | HY-106994 | Nebentan | 403604-85-3 | 10mg | 4000元 |
常見問題列表
|
ET A 0.697 nM (Ki) |
ET B 569 nM (Ki) |
Nebentan 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 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.
Nebentan (oral administration; 0.1-1 mg/kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy.Nebentan (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.