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.

HIF-PHD-IN-1 (compound 19) (0.5-2 mg/kg; p. o. once daily for 4 weeks) improves hemoglobin levels in anemic rats[1]. HIF-PHD-IN-1 (10 mg/kg; single p.o.) increases serum erythropoietin (EPO) concentration at 8 h after administration in SD rats[1]. HIF-PHD-IN-1 (1 mg/kg; p.o.) shows good bioavailability (F=77%) in male SD rats[1]. Animal Model: Male SD Rats excising ?ve-sixths of their kidneys[1]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[1]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%.

1567657-46-8

C17H12Cl2N6O3

419.22

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years