Nebentan potassium

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Nebentan potassium (YM598) 是一种有效的具有口服活性的非肽类内皮素受体 (ETA receptor) 拮抗剂，通过 Bosentan (HY-A0013) 修饰得到。Nebentan potassium 抑制 [125I] 内皮素-1 与人内皮素 ETA 和 ETB 受体结合，Ki 分别为 0.697 nM 和 569 nM。Nebentan potassium 可用于改善肺心病和心肌梗死的相关研究。

Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). 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. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.

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.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.

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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GPCR/G Protein

Endothelin Receptor

Endothelin Receptor

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342005-82-7

529.61

C24H20KN5O5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (236.02 mM; 超声助溶 )

O=S([N-]C1=NC(C2=NC=CC=N2)=NC(OC)=C1OC3=C(C=CC=C3)OC)(/C=C/C4=CC=CC=C4)=O.[K+]

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(-20℃)

With Ice Pack

≥ 2 years