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PF-06928215 [2378173-15-8]

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Referencia NB-64-03814-5mg

embalaje : 5mg

Marca : Neo Biotech

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PF-06928215

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Synonyms:

Catalog No. T12432 Copy Product Info

Purity: 98.95%

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

Cas No. 2378173-15-8

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.95%

Appearance:Solid

Color:White

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 Weight	380.4
Formula	C₂₀H₂₀N₄O₄
Cas No.	2378173-15-8
Smiles	OC(=O)[C@@H]1CCCC[C@@H]1NC(=O)c1cnn2c(O)cc(nc12)-c1ccccc1
Relative Density.	no data available

Storage & Solubility Information

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: 150 mg/mL (394.32 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (26.29 mM), Suspension.

10% DMSO+90% Saline: < 10 mg/mL (26.29 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

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

	1mg	5mg	10mg	50mg
1 mM	2.6288 mL	13.1441 mL	26.2881 mL	131.4406 mL
5 mM	0.5258 mL	2.6288 mL	5.2576 mL	26.2881 mL
10 mM	0.2629 mL	1.3144 mL	2.6288 mL	13.1441 mL
20 mM	0.1314 mL	0.6572 mL	1.3144 mL	6.5720 mL
50 mM	0.0526 mL	0.2629 mL	0.5258 mL	2.6288 mL
100 mM	0.0263 mL	0.1314 mL	0.2629 mL	1.3144 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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.

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.

Dose Conversion

Keywords

PF-06928215PF06928215PF 06928215InhibitorinhibitCyclic GMP-AMP SynthasecGAS

Related Tags: PF-06928215 chemical structure | PF-06928215 formula | PF-06928215 molecular weight