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E2730

(Synonyms: E 2730) Copy Product Info
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Synonyms: E 2730

Catalog No. T79399 Copy Product Info
Purity: 98.54%
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E2730 is an orally active, selective, and non-competitive GABA transporter 1 (GAT1) inhibitor with antiepileptic activity, used in neurological disease research.
E2730
Cas No. 1520073-91-9
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Pack SizePriceUSA StockGlobal StockQuantity
1 mg$293-In Stock
5 mg$722-In Stock
10 mg$987-In Stock
25 mg$1,520-In Stock
50 mg$1,980-In Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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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

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Keywords

Related Tags: E2730 chemical structure | E2730 in vivo | E2730 in vitro | E2730 formula | E2730 molecular weight