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(E)-GABAB receptor antagonist 1

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Catalog No. T11137Cas No. 1611483-29-4

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist that decreases GABA-induced IP3 (inositol trisphosphate) production with an IC50 of 37.9 μM. It is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

(E)-GABAB receptor antagonist 1

(E)-GABAB receptor antagonist 1

🥰Excellent
Purity: 98.09%
Catalog No. T11137Cas No. 1611483-29-4
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist that decreases GABA-induced IP3 (inositol trisphosphate) production with an IC50 of 37.9 μM. It is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$70In StockIn Stock
5 mg$161In StockIn Stock
10 mg$237In StockIn Stock
25 mg$355In StockIn Stock
50 mg$497In StockIn Stock
100 mg$678In StockIn Stock
1 mL x 10 mM (in DMSO)$155In 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.
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Purity:98.09%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist that decreases GABA-induced IP3 (inositol trisphosphate) production with an IC50 of 37.9 μM. It is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.
In vitro
(E)-GABAB receptor antagonist 1 decreases the maximum IP3 effect in HEK293 cells overexpressing the GABAB receptor and Gqi9 protein when induced by the agonist GABA, but does not change the EC50[1].
Chemical Properties
Molecular Weight304.38
FormulaC18H24O4
Cas No.1611483-29-4
SmilesC(=C/C(C(O)=O)=O)\C1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1
Relative Density.1.125 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: 50 mg/mL (164.27 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.2854 mL16.4268 mL32.8537 mL164.2683 mL
5 mM0.6571 mL3.2854 mL6.5707 mL32.8537 mL
10 mM0.3285 mL1.6427 mL3.2854 mL16.4268 mL
20 mM0.1643 mL0.8213 mL1.6427 mL8.2134 mL
50 mM0.0657 mL0.3285 mL0.6571 mL3.2854 mL
100 mM0.0329 mL0.1643 mL0.3285 mL1.6427 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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2 Enter the in vivo formulation:
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%
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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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