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A-484954

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Catalog No. TQ0137Cas No. 142557-61-7
Alias A 484954

A-484954 (A 484954) is a highly specific eukaryotic elongation factor-2 (eEF2, IC50: 280 nM) inhibitor.

A-484954

A-484954

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Purity: 99.86%
Catalog No. TQ0137Alias A 484954Cas No. 142557-61-7
A-484954 (A 484954) is a highly specific eukaryotic elongation factor-2 (eEF2, IC50: 280 nM) inhibitor.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$36In StockIn Stock
2 mg$51In StockIn Stock
5 mg$80In StockIn Stock
10 mg$147In StockIn Stock
25 mg$322In StockIn Stock
50 mg$572-In Stock
100 mg$815-In Stock
1 mL x 10 mM (in DMSO)$105In StockIn Stock
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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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Purity:99.86%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
A-484954 (A 484954) is a highly specific eukaryotic elongation factor-2 (eEF2, IC50: 280 nM) inhibitor.
Targets&IC50
eEF2:280 nM
In vitro
A-484954 is a selective eEF2K inhibitor and little activity against a wide panel of serine/threonine and tyrosine kinases. In the enzymatic assay, the IC50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin [1].
In vivo
Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation [2]. A484954 causes relaxation in E (+) and E (-) aorta or mesenteric artery precontracted with NA. Pretreatment with L-NAME but not indomethacin or cimetidine partially inhibits the A484954-induced relaxation in mesenteric artery [3].
SynonymsA 484954
Chemical Properties
Molecular Weight289.29
FormulaC13H15N5O3
Cas No.142557-61-7
SmilesCCn1c(=O)n(C2CC2)c2nc(N)c(cc2c1=O)C(N)=O
Relative Density.1.522 g/cm3 at 20℃
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: Insoluble
DMSO: 24.5 mg/mL (84.69 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.91 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 mM3.4567 mL17.2837 mL34.5674 mL172.8369 mL
5 mM0.6913 mL3.4567 mL6.9135 mL34.5674 mL
10 mM0.3457 mL1.7284 mL3.4567 mL17.2837 mL
20 mM0.1728 mL0.8642 mL1.7284 mL8.6418 mL
50 mM0.0691 mL0.3457 mL0.6913 mL3.4567 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

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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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