ET receptor antagonist 1 

ET receptor antagonist 1 (compound 16h) is an orally active ET receptor antagonist (IC₅₀=0.18 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 1 attenuates monocrotaline (HY-N0750) induced PAH in rat model^[1].

IC50: 0.18 nM (ET receptor)^[1]

ET receptor antagonist 1 (compound 16h) (150 mg/kg/d, 300 mg/kg/d; po; 48 h following MCT administration, for 21-26 d) results significant reduction in mPAP, and decreases the levels of HIF1α, ANP, and TNNI3 in MCT-exposed rats. And shows antioxidant profile and inhibits lipid peroxidation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

459.52

C₂₁H₂₅N₅O₅S

CC(CCOC(N=C1C2=NC=CC=N2)=C(C(NS(=O)(C)=O)=N1)OC3=CC=CC=C3OC)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]