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Vigabatrin

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Catalog No. T0128Cas No. 60643-86-9
Alias Vigabatrine, Sabril

Vigabatrin (Sabril), an analogue of gamma-aminobutyric acid, is an irreversible inhibitor of 4-aminobutyrate Transaminase responsible for the catabolism of γ-aminobutyric acid.

Vigabatrin

Vigabatrin

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Purity: 99.88%
Catalog No. T0128Alias Vigabatrine, SabrilCas No. 60643-86-9
Vigabatrin (Sabril), an analogue of gamma-aminobutyric acid, is an irreversible inhibitor of 4-aminobutyrate Transaminase responsible for the catabolism of γ-aminobutyric acid.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$44In StockIn Stock
10 mg$65In StockIn Stock
25 mg$128In StockIn Stock
50 mg$218In StockIn Stock
100 mg$393In StockIn Stock
500 mg$939-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.88%
Color:White to Yellow
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Product Introduction

Vigabatrin AI Summary
Vigabatrin exhibits a broad range of bioactivities and pharmacological properties. It demonstrates significant anticonvulsive activity in bicuculline (BIC) and picrotoxin (PCR) induced seizure tests in mice, with effective doses (ED50) of 220.0 umol.kg^-1 and 210.0 umol.kg^-1, respectively. Moreover, at a dosage of 100 mg/kg, it provides sustained protection against picrotoxin-induced convulsions. In terms of metabolism, Vigabatrin has a very short half-life of 0.005 hours at a concentration of 1 mM and a dissociation constant (pKa) of 9.5. It inhibits GABA transaminase (GABA-T) activity in vivo with an IC50 value of 41,210.0 nM and increases brain GABA levels, suggesting potential implications for regulating GABA neurotransmission in the brain. The compound also shows various activities in vitro; it inhibits gamma-aminobutyric acid aminotransferase from the pig brain with a Ki of 3200000.0 nM and a K inact rate of 0.37 min^-1, as well as rat GABA-AT with a Ki of 10,000,000.0 nM. Vigabatrin exhibits inhibitory activity against several human transporters, including BSEP, MRP2, MRP3, and MRP4, with IC50 values greater than 133000.0 nM. While it indicates moderate hepatic toxicity and potential retinotoxicity in specific test conditions, it shows no significant hepatic side effects and good aqueous solubility characteristics. Additionally, Vigabatrin demonstrates significant penetration and inhibition activities related to sodium fluorescein uptake in OATP1B1 and OATP1B3-transfected CHO cells. It has been evaluated for potential antiviral activity against SARS-CoV-2, showing some level of inhibition of virus-induced cytotoxicity and 3CL-Pro protease activity. It also shows a range of potencies in bioactivity assays against various targets, including enzymes and receptors, albeit mostly with high AC50 values, indicating relatively weak interactions. Overall, Vigabatrin has shown potential in modulating GABAergic activity and various other bioactivities, but further investigation is needed to fully understand its pharmacological profile and therapeutic potential..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Vigabatrin (Sabril), an analogue of gamma-aminobutyric acid, is an irreversible inhibitor of 4-aminobutyrate Transaminase responsible for the catabolism of γ-aminobutyric acid.
SynonymsVigabatrine, Sabril
Chemical Properties
Molecular Weight129.16
FormulaC6H11NO2
Cas No.60643-86-9
SmilesNC(CCC(O)=O)C=C
Relative Density.1.108?g/mL?at 25?°C(lit.)
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: < 1 mg/mL (insoluble)
H2O: 100 mg/mL (774.23 mM), Sonication is recommended.
Solution Preparation Table
H2O
1mg5mg10mg50mg
1 mM7.7423 mL38.7117 mL77.4234 mL387.1168 mL
5 mM1.5485 mL7.7423 mL15.4847 mL77.4234 mL
10 mM0.7742 mL3.8712 mL7.7423 mL38.7117 mL
20 mM0.3871 mL1.9356 mL3.8712 mL19.3558 mL
50 mM0.1548 mL0.7742 mL1.5485 mL7.7423 mL
100 mM0.0774 mL0.3871 mL0.7742 mL3.8712 mL

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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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