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Tiagabine GABA Receptor inhibitor

Cat.No.S4675

Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
Tiagabine GABA Receptor inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 375.55

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Quality Control

Batch: Purity: 99.56%
99.56

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (199.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 75 mg/mL

Ethanol : 75 mg/mL

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In vivo
Batch:

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 375.55 Formula

C20H25NO2S2

 Storage (From the date of receipt) 2 years 4°C liquid
CAS No. 115103-54-3 Download SDF Storage of Stock Solutions

Synonyms Gabitril, NO050328, NO328, TGB Smiles CC1=C(SC=C1)C(=CCCN2CCCC(C2)C(=O)O)C3=C(C=CS3)C

Mechanism of Action

Targets/IC50/Ki
GABA reuptake
In vitro
Tiagabine is a potent inhibitor of GABA uptake into neurons and glial cells. It is involved in modulating GABA levels, especially in areas such as the hippocampus and thalamus. This compound not only affected the decay kinetics of the IPSCs, it also reduced the frequency of occurrence of both spontaneous and miniature IPSCs.
In vivo
Tiagabine offers a significant neuroprotection in global ischemia in gerbils when given 30 min before ischemia but not when given 3 h after ischemia.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04455841 Recruiting
Anemia|Post-essential Thrombocythemia Myelofibrosis|Post-polycythemia Vera Myelofibrosis
Incyte Corporation
 March 19 2021 Phase 1|Phase 2
NCT04021355 Recruiting
Obesity|Hypertension|Circadian Dysregulation|Salt; Excess
University of Alabama at Birmingham
 July 14 2020 Not Applicable
NCT01904487 Completed
Alcoholism
Rajesh Narendran|University of Pittsburgh
 April 19 2011 Phase 1

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