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342005-82-7

英文名稱 Nebentan potassium
CAS 342005-82-7
分子式 C24H22KN5O5S
分子量 531.63
MOL 文件 342005-82-7.mol
更新日期 2023/03/20 15:41:25
342005-82-7 結(jié)構(gòu)式 342005-82-7 結(jié)構(gòu)式

基本信息

英文別名
Nebentan potassium

物理化學性質(zhì)

儲存條件-20°C儲存
溶解度DMSO: 125 mg/mL (236.02 mM)
形態(tài)Solid
顏色Off-white to light yellow

常見問題列表

生物活性
Nebentan potassium (YM598) 是一種有效的具有口服活性的非肽類內(nèi)皮素受體 (ETA receptor) 拮抗劑,通過 Bosentan (HY-A0013) 修飾得到。Nebentan potassium 抑制 [125I] 內(nèi)皮素-1 與人內(nèi)皮素 ETA 和 ETB 受體結(jié)合,Ki 分別為 0.697 nM 和 569 nM。Nebentan potassium 可用于改善肺心病和心肌梗死的相關(guān)研究。
靶點

ET A

0.679 nM (Ki)

ET B

569 nM (Ki)

體外研究

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.

體內(nèi)研究

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.

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