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Bicyclo-GABA
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Catalog No. T218115 Copy Product Info
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Bicyclo-GABA is a selective competitive non-transportable inhibitor of the betaine/GABA transporter 1 (BGT1) with an IC50 of 590 nM. It exhibits low micromolar agonist activity at α1β2γ2GABAA receptors, with an EC50 of 5.1 μM. Bicyclo-GABA demonstrates activity that is 129 times higher for BGT1 than for GAT3. As a valuable tool compound, Bicyclo-GABA aids in elucidating its pharmacological role in both the central and peripheral nervous systems.
Bicyclo-GABA
Cas No. 1615763-33-1
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Bicyclo-GABA is a selective competitive non-transportable inhibitor of the betaine/GABA transporter 1 (BGT1) with an IC50 of 590 nM. It exhibits low micromolar agonist activity at α1β2γ2GABAA receptors, with an EC50 of 5.1 μM. Bicyclo-GABA demonstrates activity that is 129 times higher for BGT1 than for GAT3. As a valuable tool compound, Bicyclo-GABA aids in elucidating its pharmacological role in both the central and peripheral nervous systems. |
| In vitro | Bicyclo-GABA effectively inhibits the uptake of [3H]GABA by human BGT1 within a concentration range of 0.1-10,000 nM for 3 minutes, with an IC50 of 1.5 μM. It acts as a non-transportable competitive inhibitor of human BGT1, with a K B of 0.47 μM when used in concentrations ranging from 0-10 μM. Bicyclo-GABA also exhibits agonistic activity on human α1β2γ2 GABA A receptors, with an EC50 of 5.1 μM at concentrations of 0.01-100 μM. Additionally, in cell-based [3H]GABA uptake assays, Bicyclo-GABA modulates inhibitory activity on BGT1 and GAT3 mutants, with IC50 values ranging from 0.040 to 610 μM. |
| Molecular Weight | 141.17 |
| Formula | C7H11NO2 |
| Cas No. | 1615763-33-1 |
| Smiles | N[C@]12[C@]([C@@H](C(O)=O)CC1)(C2)[H] |
| Storage | 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:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
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 DMSO 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 DMSO stock solution to 400 µL PEG300 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 ddH2O 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.
Dose Conversion
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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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Related Tags: Bicyclo-GABA in vitro | Bicyclo-GABA formula | Bicyclo-GABA molecular weight
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