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ESI-09

🥰Excellent
Catalog No. T2244Cas No. 263707-16-0

ESI-09 is a new-typel noncyclic nucleotide EPAC antagonist.The IC50 values of ESI-09 for EPAC1 and EPAC2 is 3.2 and 1.4 μM, respectively.

ESI-09

ESI-09

🥰Excellent
Purity: 99.57%
Catalog No. T2244Cas No. 263707-16-0
ESI-09 is a new-typel noncyclic nucleotide EPAC antagonist.The IC50 values of ESI-09 for EPAC1 and EPAC2 is 3.2 and 1.4 μM, respectively.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$35In StockIn Stock
5 mg$56In StockIn Stock
10 mg$89In StockIn Stock
25 mg$177In StockIn Stock
50 mg$320In StockIn Stock
100 mg$482In StockIn Stock
1 mL x 10 mM (in DMSO)$61In 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:99.57%
Color:White to Yellow
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Product Introduction

Bioactivity
Description
ESI-09 is a new-typel noncyclic nucleotide EPAC antagonist.The IC50 values of ESI-09 for EPAC1 and EPAC2 is 3.2 and 1.4 μM, respectively.
Targets&IC50
EPAC1:3.2 μM, EPAC2:1.4 μM
In vitro
In WT C57BL/6 mice, ESI-09 (10 mg/kg/d, i.p.) prevents SFG Rickettsiosis by inhibiting EPAC1.
In vivo
ESI-09 specifically inhibits intracellular EPAC-mediated activation of Rap1 and phosphorylation of Akt, as well as EPAC-mediated secretion in pancreatic β-cells. In pancreatic cancer cells induced by 007-AM, ESI-09 reduces cell adhesion and inhibits cell migration. In Schwann cells stimulated by CPT-cAMP, ESI-09 significantly suppresses cell differentiation and myelination. Additionally, in SC neuronal cultures, ESI-09 notably decreases the number of O1-positive and MBP-positive cells.
Chemical Properties
Molecular Weight330.77
FormulaC16H15ClN4O2
Cas No.263707-16-0
SmilesCC(C)(C)c1cc(no1)C(=O)C(=NNc1cccc(Cl)c1)C#N
Relative Density.no data available
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 83.33 mg/mL (251.93 mM), Sonication is recommended.
Ethanol: 6.6 mg/mL (19.95 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.05 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
Ethanol/DMSO
1mg5mg10mg50mg
1 mM3.0232 mL15.1162 mL30.2325 mL151.1624 mL
5 mM0.6046 mL3.0232 mL6.0465 mL30.2325 mL
10 mM0.3023 mL1.5116 mL3.0232 mL15.1162 mL
DMSO
1mg5mg10mg50mg
20 mM0.1512 mL0.7558 mL1.5116 mL7.5581 mL
50 mM0.0605 mL0.3023 mL0.6046 mL3.0232 mL
100 mM0.0302 mL0.1512 mL0.3023 mL1.5116 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

Keywords

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