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HIF-PHD-IN-1
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Catalog No. T39040Cas No. 1567657-46-8
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.
HIF-PHD-IN-1
🥰Excellent
Catalog No. T39040Cas No. 1567657-46-8
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.
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| Description | 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. |
| Targets&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, enhances hemoglobin levels in anemic rats, indicating potential effectiveness in treating anemia. A single oral dose of 10 mg/kg significantly increases serum erythropoietin (EPO) levels 8 hours post-administration in Sprague-Dawley (SD) rats, suggesting a stimulatory effect on erythropoiesis. At 1 mg/kg, HIF-PHD-IN-1 shows good bioavailability (F=77%) in male SD rats, indicating efficient absorption. This study used male SD rats with five-sixths nephrectomy to simulate anemia. The results show improved hemoglobin levels starting at weeks 2 and 1 for the 1 and 2 mg/kg/day groups, respectively. Pharmacokinetic analysis at 1 mg/kg, administered orally or intravenously, showed Cmax values of 1839 ng/mL (oral) and 12357 ng/mL (intravenous), with a bioavailability of 77%. |
| Molecular Weight | 419.22 |
| Formula | C17H12Cl2N6O3 |
| Cas No. | 1567657-46-8 |
| Smiles | C[C@@H](c1cc(Cl)ccc1Cl)n1ncc2nc([nH]c(=O)c12)-n1cc(cn1)C(O)=O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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