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MK-8617
🥰Excellent
Catalog No. T4106Cas No. 1187990-87-9
Alias MK8617
MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM).
MK-8617
🥰Excellent
Purity: 99.38%
Catalog No. T4106Alias MK8617Cas No. 1187990-87-9
MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $40 | In Stock | In Stock | |
| 10 mg | $68 | In Stock | In Stock | |
| 25 mg | $148 | In Stock | In Stock | |
| 50 mg | $248 | In Stock | In Stock | |
| 100 mg | $413 | In Stock | In Stock | |
| 200 mg | $589 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.38%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM). |
| Targets&IC50 | PHD3:14 nM, PHD2:1 nM, PHD1:1 nM |
| In vitro | In vitro, MK-8617 hasn't markedly inhibitory for CYP1A2, 3A4, 2B6, 2C9, 2C19, or 2D6 (IC50>60 μM), and is a moderate reversible inhibitor of CYP2C8 (IC50: 1.6 μM). MK-8617 (10 μM) is inactive against a general panel of 171 radioligand binding and enzymatic assays. |
| In vivo | In liver microsomes (+NADPH) from rat, dog, and monkey, tritiated MK-8617 exhibits minimal metabolic turnover (<10%), but the significant turnover (34%) in HLMs after 60 min (10 μM compound, 1 mg/mL microsomal protein). MK-8617 has good oral bioavailability across species (36?71%), with low clearance and volume of distribution. Increases in circulating reticulocytes are observed at 5 and 15 mg/kg 3 days after challenge and at the 15 mg/kg 4 days after challenge. |
| Synonyms | MK8617 |
| Molecular Weight | 443.45 |
| Formula | C24H21N5O4 |
| Cas No. | 1187990-87-9 |
| Smiles | COc1ccc(cc1)C(NC(=O)c1cnc([nH]c1=O)-c1cccnn1)c1ccc(OC)cc1 |
| Relative Density. | 1.32 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||
| Solubility Information | DMSO: 1 mg/mL (2.26 mM), Sonication is recommended.  | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
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Calculator
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.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
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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