产品
编 号:F745841
分子式:C17H12Cl2N6O3
分子量:419.22
产品类型
结构图
CAS No: 1567657-46-8
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产品详情
生物活性:
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.
体内研究:
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.Animal Model:Male SD Rats excising ?ve-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:Cmax=1839 ng/mL (p.o.); Cmax=12357ng/mL (i.v.); F=77%.