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CAS No. : 342005-82-7
MCE 国际站:Nebentan potassium
产品活性: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。
研究领域:GPCR/G Protein
作用靶点:Endothelin Receptor
In Vitro: 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.
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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cardiovascular Disease Compound Library | Neurotransmitter Receptor Compound Library | Angiogenesis-Related Compound Library | Targeted Diversity Library | Anti-Prostate Cancer Compound Library | Coagulation and Anti-coagulation Compound Library | Heterocyclic Compound Library | Pain-Related Compound Library | Antihypertensive Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | BQ-788 | [Asn18] Endothelin-1, human | TBC3711 | BQ-3020 TFA | Sparsentan | [Lys4] Sarafotoxin S6c | Bosentan | Endothelin 1 (swine, human) (TFA) | Ambrisentan | Ro 46-2005 | [Ala2] Endothelin-3, human | ZD-1611 | PD-159020 | Aminaftone | A-192621 | Macitentan | Sulfisoxazole | Endothelin-3, human, mouse, rabbit, rat TFA | IRL 2500 | Carperitide acetate | Atrial Natriuretic Peptide (ANP) (1-28), rat TFA | ACT-373898 | Kendomycin | Zibotentan | BQ-123 TFA
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