AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor ) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a K i of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes.