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PF-06928215

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Catalog No. T12432Cas No. 2378173-15-8

PF-06928215 is an inhibitor of cGAS (cyclic GMP-AMP Synthase) (IC50 of 4.9 μΜ).

PF-06928215

PF-06928215

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🥰Excellent
Purity: 98.95%
Catalog No. T12432Cas No. 2378173-15-8
PF-06928215 is an inhibitor of cGAS (cyclic GMP-AMP Synthase) (IC50 of 4.9 μΜ).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$77In StockIn Stock
5 mg$189In StockIn Stock
10 mg$278In StockIn Stock
25 mg$528In StockIn Stock
50 mg$769In StockIn Stock
100 mg$1,080In StockIn Stock
1 mL x 10 mM (in DMSO)$198In 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:98.95%
Appearance:Solid
Color:White
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Product Introduction

PF-06928215 AI Summary
PF-06928215 exhibits bioactivity related to the inhibition of human cGAS, specifically targeting the reduction in cGAMP levels when expressed in Sf9 insect cells. It shows a strong binding affinity with a measured dissociation constant (Kd) of 200.0 nM, as determined by various methods, including fluorescence polarization assays and surface plasmon resonance analysis. The compound also demonstrates inhibitory effects with IC50 values of 4900.0 nM and 2000.0 nM in different assays assessing cGAMP reduction levels using ISD DNA as a substrate in the presence of ATP and GTP..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
PF-06928215 is an inhibitor of cGAS (cyclic GMP-AMP Synthase) (IC50 of 4.9 μΜ).
Targets&IC50
cGAS:4.9 μM
Chemical Properties
Molecular Weight380.4
FormulaC20H20N4O4
Cas No.2378173-15-8
SmilesOC(=O)[C@@H]1CCCC[C@@H]1NC(=O)c1cnn2c(O)cc(nc12)-c1ccccc1
Relative Density.no data available
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: 150 mg/mL (394.32 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.63 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6288 mL13.1441 mL26.2881 mL131.4406 mL
5 mM0.5258 mL2.6288 mL5.2576 mL26.2881 mL
10 mM0.2629 mL1.3144 mL2.6288 mL13.1441 mL
20 mM0.1314 mL0.6572 mL1.3144 mL6.5720 mL
50 mM0.0526 mL0.2629 mL0.5258 mL2.6288 mL
100 mM0.0263 mL0.1314 mL0.2629 mL1.3144 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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

Keywords

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