PHD2-IN-1, a potent and orally active HIF prolyl hydroxylase 2 (PHD2) inhibitor, exhibits an IC50 of 22.53 nM and is applicable in anemia research [1].

PHD2-IN-1 (Compound 22), at concentrations ranging from 0-50 µM and applied over a period of 12 hours, stabilizes HIF-α and enhances the expression of the erythropoietin (EPO) gene.

PHD2-IN-1 (Compound 22) administered orally at 10, 20, and 50 mg/kg once daily for three consecutive days stimulated erythropoiesis and increased reticulocyte counts in a dose-dependent manner in C57BL/6 mice [1]. When injected intraperitoneally at 50, 100, and 200 mg/kg in ICR mice, it exhibited no significant toxic responses after three days of once-daily administration [1]. Pharmacokinetic analysis indicated that PHD2-IN-1 has a half-life (T 1/2) of 2.29 hours orally and 3.72 hours intravenously in rats, and 1.17 hours orally and 0.33 hours intravenously in mice, with oral bioavailability (F%) of 33.9% in rats and 35.3% in mice [1]. Pharmacokinetic parameters for PHD2-IN-1 in SD rats and C57BL/6 mice, including Tmax, Cmax, AUC0-t, AUC0-∞, T 1/2, clearance (CL), volume of distribution (Vz), mean residence time (MRT), and bioavailability (F%) across different administration routes and dosages, are summarized in the provided table [1].