research use only

Tiagabine hydrochloride GABA Receptor inhibitor

Name: Tiagabine hydrochloride
Brand: Selleck Chemicals
SKU: S4661
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4661

Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.

Chemical Structure

Molecular Weight: 412.01

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S466101 DMSO]82 mg/mL]false]Ethanol]82 mg/mL]false]Water]11 mg/mL]false Purity: 99.78%

99.78

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor TRP Channel Cholinesterase (ChE) GluR MAO Beta Amyloid NMDAR iGluR P2 Receptor Trk receptor Serotonin Transporter Notch Norepinephrine Cannabinoid Receptor P-gp CaMK Opioid Receptor BACE Sigma Receptor FAAH Neurokinin Receptor OX Receptor CGRP Receptor CCK receptor
Related Products	Dihydromyricetin CGP52432 Ginkgolide A 4-Aminobutyric acid (GABA) SR95531 Chinese Arborvilea Seed Extract Afoxolaner Homotaurine (+)-Borneol L-DAB HBR 6-Hydroxyflavone (6-HF) Valepotriate Nefiracetam (1S)-(-)-α-Pinene Securinine Phenibut Phaclofen Pentylenetetrazol GABA B Receptor 2/GABBR2 Antibody [G13F10] Piracetam Crateva nurvala Extract Arecaidine hydrochloride AZD6280 GABA B Receptor 1 Antibody [B13L23] 3,4,5-Trimethoxycinnamic acid Afloqualone p-Hydroxybenzaldehyde (2S)-6-Prenylnaringenin GABAA receptor agent 1 Bemegride

Chemical Information, Storage & Stability

Molecular Weight	412.01	Formula	C₂₀H₂₅NO₂S₂.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	145821-59-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Gabitril hydrochloride, NO050328 hydrochloride, NO328 hydrochloride, TGB hydrochloride			Smiles	CC1=C(SC=C1)C(=CCCN2CCCC(C2)C(=O)O)C3=C(C=CS3)C.Cl

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (199.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 82 mg/mL

Water : 11 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.1mg/ml (9.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 82 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.58mg/ml (1.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 11.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	GABA uptake ^[1]
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^[2]. Tiagabine not only affected the decay kinetics of the IPSCs, it also reduced the frequency of occurrence of both spontaneous and miniature IPSCs^[4].
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^[3].
References	[1] https://pubmed.ncbi.nlm.nih.gov/9125411/ [2] https://pubmed.ncbi.nlm.nih.gov/12608706/ [3] https://pubmed.ncbi.nlm.nih.gov/12137918/ [4] https://pubmed.ncbi.nlm.nih.gov/12879169/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):