HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD) , with an IC 50 of 54 nM for hHIF-PHD2 . HIF-PHD-IN-1 is promising therapeutic agents for renal anemia
In Vivo
HIF-PHD-IN-1 (compound 19) (0.5-2 mg/kg; p. o. once daily for 4 weeks) improves hemoglobin levels in anemic rats . HIF-PHD-IN-1 (10 mg/kg; single p.o.) increases serum erythropoietin (EPO) concentration at 8 h after administration in SD rats . HIF-PHD-IN-1 (1 mg/kg; p.o.) shows good bioavailability (F=77%) in male SD rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male SD Rats excising five-sixths of their kidneys Dosage: 0.5, 1, 2 mg/kg Administration: P.o. once daily for 4 weeks Result: Improved blood hemoglobin levels starting at weeks 2 and 1 in the groups receiving 1 and 2 (mg/kg)/day, respectively. Animal Model: Male SD Rats Dosage: 1 mg/kg (Pharmacokinetic Analysis) Administration: Single p.o. or i.v. Result: C max =1839 ng/mL (p.o.); C max =12357ng/mL (i.v.); F=77%.
