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GSK-239512

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Catalog No. T27462Cas No. 720691-69-0
Alias GSK239512, GSK 239512

GSK-239512 is an antagonist of H3 receptor and can be used in studies about the treatment of cognitive dysfunction in neurodegenerative disorders.

GSK-239512

GSK-239512

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Purity: 99.74%
Catalog No. T27462Alias GSK239512, GSK 239512Cas No. 720691-69-0
GSK-239512 is an antagonist of H3 receptor and can be used in studies about the treatment of cognitive dysfunction in neurodegenerative disorders.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$39In StockIn Stock
5 mg$87In StockIn Stock
10 mg$115In StockIn Stock
25 mg$198In StockIn Stock
50 mg$297In StockIn Stock
100 mg$448-In Stock
1 mL x 10 mM (in DMSO)$94In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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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Batch Information

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Purity:99.74%
Appearance:Solid
Color:White to Yellow
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Product Introduction

GSK-239512 AI Summary
GSK-239512 exhibits a variety of bioactivities. It shows high binding affinity to human serum albumin, with 75.0% inhibition, and a time-dependent inhibition of CYP450. The compound possesses high oral bioavailability in different animal models and displays favorable terminal half-lives and peak plasma concentrations in various dosing regimens. Notably, it demonstrates potent ex vivo binding affinity to histamine H3 receptors in both rat and human tissues, with low Ki values. It shows antagonist activity at the human histamine H3 receptor, with a Ki of 0.1 nM for GTPgammaS binding inhibition, and a binding affinity of Ki = 10.0 nM to the recombinant human H3 receptor, suggesting strong inhibitory effects and potential in modulating H3 receptor function..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
GSK-239512 is an antagonist of H3 receptor and can be used in studies about the treatment of cognitive dysfunction in neurodegenerative disorders.
SynonymsGSK239512, GSK 239512
Chemical Properties
Molecular Weight377.48
FormulaC23H27N3O2
Cas No.720691-69-0
SmilesO=C1CCCN1c1ccc(Oc2ccc3CCN(CCc3c2)C2CCC2)nc1
Relative Density.1.239 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: 6.9 mg/mL (18.28 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6491 mL13.2457 mL26.4915 mL132.4573 mL
5 mM0.5298 mL2.6491 mL5.2983 mL26.4915 mL
10 mM0.2649 mL1.3246 mL2.6491 mL13.2457 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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g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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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