PeptideDB

ET receptor antagonist 2

CAS: F: C22H25N5O5S W: 471.53

ET receptor antagonist 2 (compound 16j) is an orally active ET receptor antagonist (IC50=0.22 nM), which can be used for
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This product is for research use only, not for human use. We do not sell to patients.

Bioactivity ET receptor antagonist 2 (compound 16j) is an orally active ET receptor antagonist (IC50=0.22 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 2 attenuates monocrotaline (HY-N0750) induced PAH in rat model[1].
Target IC50: 0.22 nM (ET receptor)
In Vivo ET receptor antagonist 2 (compoud 16j) (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 2
Formula C22H25N5O5S
Molar Mass 471.53
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.