Bioactivity | ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 3 attenuates monocrotaline (HY-N0750) induced PAH in rat model[1]. |
Target | IC50: 0.26 nM (ET receptor) |
In Vivo | ET receptor antagonist 3 (compound 17d) (150 mg/kg/d, 300 mg/kg/d; 口服; MCT 处理后 48 h 开始给药, 共 21-26 d) 显著降低 MCT 暴露大鼠的 mPAP 水平,降低 HIF1α、ANP、TNNI3水平。显示出抗氧化和抑制脂质过氧化作用[1]。 |
Name | ET receptor antagonist 3 |
Formula | C27H28N6O5S |
Molar Mass | 548.61 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Panchal J, et al. Development of novel bosentan analogues as endothelin receptor antagonists for pulmonary arterial hypertension. Eur J Med Chem. 2023 Nov 5;259:115681. |