Molidustat

Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC₅₀ values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia^[1][2]. IC50 & Target:IC50: 480 nM (PHD1), 280 nM (PHD2), 450 nM (PHD3)^[1] In Vitro:Molidustat (BAY 85-3934) (5 μM; 20 min) is sufficient to induce detectable levels of HIF-1α in HeLa cells. In a cell reporter assay, Molidustat induces expression of a firefly luciferase reporter gene under the control of a hypoxia response element promoter with a mean (± SD) EC50 of 8.4 μM (n=4)^[1]. In Vivo:Molidustat (BAY 85-3934) , by stabilizing the hypoxia-inducible factor (HIF), leads to a dose-dependent increase in erythropoietin (EPO) in both Wistar rats (0.5-5 mg/kg; oral; once daily for 26 days) and cynomolgus monkeys (0.5-1.5mg/kg; once daily for 5 days)^[1].
Molidustat (0.5-10 mg/kg; orally; five times weekly) can normalize the blood pressure in rat models of chronic kidney disease (CKD) and effectively alleviate renal anemia in rats with impaired renal function^[1].