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PF-04937319

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Catalog No. T16479Cas No. 1245603-92-2

PF-04937319 is an activator of glucokinase (EC50 =154.4  μM). PF-04937319 maintains glucose-lowering efficacy while mitigating the risk of hypoglycemia observed with many other glucokinase activators. PF-04937319 can be used in research on the treatment of type 2 diabetes mellitus.

PF-04937319

PF-04937319

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🥰Excellent
Purity: 99.89%
Catalog No. T16479Cas No. 1245603-92-2
PF-04937319 is an activator of glucokinase (EC50 =154.4  μM). PF-04937319 maintains glucose-lowering efficacy while mitigating the risk of hypoglycemia observed with many other glucokinase activators. PF-04937319 can be used in research on the treatment of type 2 diabetes mellitus.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$38In StockIn Stock
5 mg$89In StockIn Stock
10 mg$155In StockIn Stock
25 mg$322In StockIn Stock
50 mg$587In StockIn Stock
100 mg$855In StockIn Stock
1 mL x 10 mM (in DMSO)$98In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.89%
Appearance:Solid
Color:White
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Product Introduction

PF-04937319 AI Summary
PF-04937319 is a multifaceted bioactive compound demonstrating diverse biological activities across several systems. It notably activates human recombinant glucokinase and promotes glucokinase translocation from the nucleus to the cytoplasm in rat hepatocytes. The compound shows enhanced drug uptake via human hepatic OATP1B1 and OATP1B3 transporters and possesses apparent permeability across dog RRCK cells. Its lipophilicity, with a LogD7.4 value of 2.1, suggests favorable bioavailability and interaction potential with lipid bilayers. In pharmacokinetic studies, PF-04937319 exhibits a high fraction unbound in rat plasma. It shows activation of glucokinase by increasing enzyme velocity and altering the glucokinase Km, with an EC50 of 190.0 nM in a glucose-present assay. The compound also demonstrates antidiabetic potential in Sprague-Dawley rats and exhibits a therapeutic index greater than 5.0. It has demonstrated antiviral activity against SARS-CoV-2, reducing cytotoxicity in Caco-2 and VERO-6 cells at a concentration of 10 μM, although with varying inhibitory percentages. Additionally, PF-04937319 shows inhibition of the SARS-CoV-2 3CL-Pro protease and exhibits minor inhibitory activity on human HDAC6. With its diverse bioactivities, particularly in glucose metabolism regulation, antiviral properties, and high permeability, PF-04937319 is a promising candidate for further pharmacological exploration..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
PF-04937319 is an activator of glucokinase (EC50 =154.4  μM). PF-04937319 maintains glucose-lowering efficacy while mitigating the risk of hypoglycemia observed with many other glucokinase activators. PF-04937319 can be used in research on the treatment of type 2 diabetes mellitus.
Targets&IC50
GK:154.4 μM(EC50)
Chemical Properties
Molecular Weight432.43
FormulaC22H20N6O4
Cas No.1245603-92-2
SmilesCN(C)C(=O)c1ncc(Oc2cc(cc3oc(C)cc23)C(=O)Nc2cnc(C)cn2)cn1
Relative Density.1.366 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 95 mg/mL (219.69 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3125 mL11.5626 mL23.1251 mL115.6257 mL
5 mM0.4625 mL2.3125 mL4.6250 mL23.1251 mL
10 mM0.2313 mL1.1563 mL2.3125 mL11.5626 mL
20 mM0.1156 mL0.5781 mL1.1563 mL5.7813 mL
50 mM0.0463 mL0.2313 mL0.4625 mL2.3125 mL
100 mM0.0231 mL0.1156 mL0.2313 mL1.1563 mL

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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