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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
Other Forms of (E)-GABAB receptor antagonist 1:
GABAB receptor antagonist 1T11350797-17-1
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(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 SizePriceAvailabilityQuantity
1 mg$70In Stock
5 mg$161In Stock
10 mg$237In Stock
25 mg$355In Stock
50 mg$497In Stock
100 mg$678In Stock
1 mL x 10 mM (in DMSO)$155In Stock
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Bulk & Custom
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. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Batch Information

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Purity:98.09%
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COA HNMR LCMS

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 mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
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Keywords

GABAReceptorGABAB receptor antagonist 1GABAB receptorGABABGABA Receptor(E)GABAB receptor antagonist 1(E) GABAB receptor antagonist 1
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