ZG-2686 is a potent and selective HIF-2α agonist with an EC 50 of 0.25 µM. ZG-2686 exhibits selectivity over PHD2 . ZG-2686 binds to a specific internal cavity of HIF-2α, forming hydrogen bonds via structural water molecules, which stabilizes the HIF-2α/ β heterodimer and enhances transcriptional activity. ZG-2686 synergizes with Vadadustat ( HY-101277 ) to upregulate HIF-2α-dependent EPO gene expression both in vitro and in vivo. ZG-2686 can be used for the research of renal anemia.
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