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Nebentan

CAS No. : 403604-85-3

MCE 站：Nebentan

产品活性：Nebentan (YM598 free base) 是一种有效的具有口服活性的非肽类内皮素受体 (ET_A receptor) 拮抗剂，通过 Bosentan (HY-A0013) 修饰得到。Nebentan 抑制 [¹²⁵I] 内皮素-1 与人内皮素 ET_A 和 ET_B 受体结合，K_i 分别为 0.697 nM 和 569 nM。Nebentan 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 inhibits the specific binding of [¹²⁵I] 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 Ca²⁺ concentration, Nebentan 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 (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.

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  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Anti-Cardiovascular Disease Compound Library  |  Neurotransmitter Receptor Compound Library  |  Angiogenesis Related Compound Library  |  Endothelin 1 (swine, human)  |  BQ-788 sodium salt  |  Bosentan  |  Macitentan  |  BQ-123  |  Atrasentan hydrochloride  |  Sparsentan  |  Ambrisentan  |  Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate  |  Sulfisoxazole  |  Avosentan  |  Aprocitentan  |  Atrial Natriuretic Peptide (ANP) (1-28), rat  |  Zibotentan  |  Darusentan  |  Sitaxsentan sodium  |  A-192621  |  IRL 2500  |  BQ-3020 TFA  |  IRL-1620  |  Tezosentan  |  ABT-546  |  Aminaftone

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