Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HIF-PHD-IN-1 is a pharmacological compound that acts as an orally active inhibitor of the hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), displaying an IC50 of 54 nM for hHIF-PHD2. Its potential as a therapeutic agent for renal anemia is highly promising.
説明 | HIF-PHD-IN-1 is a pharmacological compound that acts as an orally active inhibitor of the hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), displaying an IC50 of 54 nM for hHIF-PHD2. Its potential as a therapeutic agent for renal anemia is highly promising. |
ターゲット&IC50 | HIF-PHD2 (human):54 nM (IC50) |
In vivo | HIF-PHD-IN-1 (compound 19), administered orally at doses of 0.5-2 mg/kg once daily for four weeks, has been shown to enhance hemoglobin levels in anemic rats, indicating its potential effectiveness in treating anemia. When given as a single oral dose of 10 mg/kg, it significantly increases serum erythropoietin (EPO) levels 8 hours post-administration in Sprague-Dawley (SD) rats, suggesting a stimulatory effect on erythropoiesis. Additionally, at a dose of 1 mg/kg, HIF-PHD-IN-1 demonstrates good bioavailability (F=77%) in male SD rats, underlining its efficient absorption. This study employed male SD rats with five-sixths of their kidneys removed to simulate anemia. The results indicate a noticeable improvement in blood hemoglobin levels commencing at weeks 2 and 1 for the 1 and 2 mg/kg/day groups, respectively. Pharmacokinetic analysis at a dosage of 1 mg/kg, administered either orally or intravenously, showed maximum concentrations (Cmax) of 1839 ng/mL (oral) and 12357 ng/mL (intravenous), with a bioavailability of 77%. |
分子量 | 419.22 |
分子式 | C17H12Cl2N6O3 |
CAS No. | 1567657-46-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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HIF-PHD-IN-1 1567657-46-8 HIFPHDIN1 HIF PHD IN 1 Inhibitor inhibitor inhibit