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. 2020 Apr 23;5(8):e132898. doi: 10.1172/jci.insight.132898

Figure 1. APJ receptor activation with small-molecule agonists and endogenous ligand.

Figure 1

(A) The chemical structure of AM-8123 and AMG 986. The APJ small-molecule agonists AM-8123 (shown in red) and AMG 986 (shown in blue) and the endogenous ligand pyr-apelin-13 (shown in black) alter (B) cAMP levels (8, 16, and 10 individual experiments for each concentration of AM-8123, AMG 986, and pyr-apelin-13, respectively) and promote binding of nonhydrolyzable (C) GTPγS (14, 24, and 16 individual experiments for each concentration of AM-8123, AMG 986, and pyr-apelin-13, respectively) in human APJ–overexpressing (hAPJ-overexpressing) cells. Both AM-8123 and AMG 986 activation of hAPJ led to (D) β-arrestin recruitment (8, 8, and 24 individual experiments for each concentration of AM-8123, AMG 986, and pyr-apelin-13, respectively) and (E) receptor internalization (24 individual experiments per group) in a dose-dependent manner. Data shown as a box-and-whisker plot with a line indicating the median, the box representing the 25th–75th interquartile range, and the whiskers, calculated with Tukey’s method.