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GSK 525768A

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Catalog No. T11472Cas No. 1260530-25-3

GSK 525768A, the inactive enantiomer of GSK525762A, exhibits no activity towards BET.

GSK 525768A
Other Forms of GSK 525768A:

GSK 525768A

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Catalog No. T11472Cas No. 1260530-25-3
GSK 525768A, the inactive enantiomer of GSK525762A, exhibits no activity towards BET.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$1986-8 weeks6-8 weeks
5 mg$3476-8 weeks6-8 weeks
25 mg$1,1706-8 weeks6-8 weeks
50 mg$1,5306-8 weeks6-8 weeks
100 mg$1,9906-8 weeks6-8 weeks
1 mL x 10 mM (in DMSO)$3826-8 weeks6-8 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction

Bioactivity
Description
GSK 525768A, the inactive enantiomer of GSK525762A, exhibits no activity towards BET.
In vitro
GSK 525768A interacts with the protein's module by establishing hydrogen bonds with the conserved asparagine residue, effectively mimicking the acetylated lysine's binding mechanism. This interaction leads to the compound's binding deeper within the acetylated lysine's binding site, all the while preserving the position of conserved water molecules in the acetyl-lysine binding cavity's base. GSK 525768A exhibits no activity towards BET and is identified as the (R)-enantiomer of GSK525762A. Contrasting its counterpart, GSK525762A, which influences the regulation of apolipoprotein A1 (APOA1) levels in liver cell assays, GSK 525768A does not impact APOA1 release, highlighting a distinctive functional divergence between the two enantiomers.
Chemical Properties
Molecular Weight423.9
FormulaC22H22ClN5O2
Cas No.1260530-25-3
SmilesCCNC(=O)C[C@H]1N=C(c2ccc(Cl)cc2)c2cc(OC)ccc2-n2c(C)nnc12
Relative Density.1.35 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: 100 mg/mL (235.9 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.78 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 mM2.3590 mL11.7952 mL23.5905 mL117.9523 mL
5 mM0.4718 mL2.3590 mL4.7181 mL23.5905 mL
10 mM0.2359 mL1.1795 mL2.3590 mL11.7952 mL
20 mM0.1180 mL0.5898 mL1.1795 mL5.8976 mL
50 mM0.0472 mL0.2359 mL0.4718 mL2.3590 mL
100 mM0.0236 mL0.1180 mL0.2359 mL1.1795 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

GSK 525768A
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