compound introduction
Information MK-8617 is an pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting PHD1 , 2 , 3 with IC50s of 1.0, 1.0 and 14 nM, respectively. Targets PHD1 (Cell-free assay); PHD2 (Cell-free assay); PHD3 (Cell-free assay) 1 nM; 1 nM; 14 nM In vitro MK-8617 is not a significant inhibitor of the cytochrome p450 enzymes in vitro (IC50), CYP1A2, 3A4, 2B6, 2C9, 2C19, or 2D6, >60 μM, and is a moderate reversible inhibitor of CYP2C8 at 1.6 μM in vitro. MK-8617 is inactive when screened at 10 μM against a general panel of 171 radioligand binding and enzymatic assays. In vivo Tritiated MK-8617 exhibits minimal metabolic turnover in liver microsomes (+NADPH) from rat, dog, and monkey (
