IC50: 54 nM (hHIF-PHD2)[1]
HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia[1].
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: | Cmax=1839 ng/mL (p.o.); Cmax=12357ng/mL (i.v.); F=77%. |
[1]. Goi T, et, al. Pyrazolo[4,3- d]pyrimidine Derivatives as a Novel Hypoxia-Inducible Factor Prolyl Hydroxylase Domain Inhibitor for the Treatment of Anemia. ACS Med Chem Lett. 2020 Jun 4; 11(7): 1416-1420.