Molidustat sodium (5 μM; 20 min) is sufficient to induce detectable levels of HIF-1α in HeLa cells. In a cellular reporter assay, the compound stimulates the expression of the luciferase reporter gene under the control of a hypoxia-responsive element promoter, with an average (± SD) EC50 of 8.4 μM (n=4).

Molidustat sodium (5 μM; 20 min) is sufficient to induce detectable levels of HIF-1α in HeLa cells. In a cellular reporter assay, the compound stimulates the expression of the luciferase reporter gene under the control of a hypoxia-responsive element promoter, with an average (± SD) EC50 of 8.4 μM (n=4).

Administered orally at doses ranging from 0.5 to 5 mg/kg once daily for 26 days in Wistar rats, and from 0.5 to 1.5 mg/kg once daily for 5 days in cynomolgus monkeys, Molidustat sodium stabilizes hypoxia-inducible factors (HIF), thereby inducing a dose-dependent increase in erythropoietin (EPO) production in both healthy Wistar rats and cynomolgus monkeys. In a chronic kidney disease (CKD) rat model, oral administration of Molidustat sodium at a dosage of 0.5-10 mg/kg five times per week normalized elevated blood pressure and effectively alleviated renal anemia associated with impaired kidney function.