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E2730

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Catalog No. T79399Cas No. 1520073-91-9
Alias E 2730

E2730 is an orally active, selective, and non-competitive GABA transporter 1 (GAT1) inhibitor with antiepileptic activity, used in neurological disease research.

E2730

E2730

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🥰Excellent
Purity: 98.54%
Catalog No. T79399Alias E 2730Cas No. 1520073-91-9
E2730 is an orally active, selective, and non-competitive GABA transporter 1 (GAT1) inhibitor with antiepileptic activity, used in neurological disease research.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$293In StockIn Stock
5 mg$722In StockIn Stock
10 mg$987In StockIn Stock
25 mg$1,520In StockIn Stock
50 mg$1,980In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
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:98.54%
ee:99.68%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
E2730 is an orally active, selective, and non-competitive GABA transporter 1 (GAT1) inhibitor with antiepileptic activity, used in neurological disease research.
Targets&IC50
GAT-1 (human):1.1 μM, BGT1 (human):890 μM
In vitro
The 50% inhibition concentration (IC50) of E2730 was 1.1 μM for hGAT1, >1000 μM for hGAT2, >1000 μM for hGAT3, and 890 μM for hBGT-1.
E2730 (0.0128-1000 μM) inhibited GAT1 in a non-competitive manner, and its inhibition was positively correlated with GABA levels in vitro. E2730 also increases extracellular GABA concentration under overactivation conditions. [1]
In vivo
E2730 (20-400mg/kg orally) showed antiepileptic effects in corneal ignition, 6 Hz-44 mA psychomotor seizures, amygdala ignition, Fragile X syndrome, and Dravet syndrome models.
The 50% effective dose (ED50) of E2730 was 7.9 mg/kg in cornea-ignited mice and the 50% toxic dose (TD50) was 350 mg/kg in accelerated rotation tests. The E2730 has a protection index (i.e. the ratio of TD50 to ED50) of 44.3. [1]
SynonymsE 2730
Chemical Properties
Molecular Weight284.23
FormulaC9H8F4N2O2S
Cas No.1520073-91-9
SmilesN(S(N)(=O)=O)[C@H]1C=2C(CC1(F)F)=CC(F)=CC2F
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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

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