TP0463518 is an orally active, competitive pan-inhibitor of hypoxia-inducible factor prolyl hydroxylases PHD1/2/3 . TP0463518 competitively inhibits human PHD1 ( IC 50 =18 nM), PHD2 (K i =5.3 nM), and PHD3 ( IC 50 =63 nM), and targets monkey PHD2 with an IC 50 of 22 nM. TP0463518 inhibits PHD-catalyzed hydroxylation to stabilize HIFα, thereby upregulating erythropoietin (EPO) expression and enhancing intestinal iron absorption (such as increased DMT-1 and dCYTb expression), improving anemia. TP0463518 is mainly used for the research of renal anemia and inflammatory anemia.
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