Art. -Nr.: HY-B0696

Tiagabine

(Synonyms: NO050328; NO328; TGB)

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Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.

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Reinheit: 99.20%
CAS. Nr.: 115103-54-3
Formel: C₂₀H₂₅NO₂S₂
Molecular Weight:375.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tiagabine Chemical Structure

CAS. Nr.: 115103-54-3

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>300 μM Compound: (R)-1a	Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis	[PMID: 25882526]
HEK293	IC₅₀	>300 μM Compound: 1, Tiagabine	Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK293 cells after 3 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK293 cells after 3 mins by scintillation counting analysis	[PMID: 23398473]
HEK293	IC₅₀	0.07 μM Compound: 5	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 25 mins by scintillation counting analysis	[PMID: 23336362]
HEK293	IC₅₀	0.64 μM Compound: 5	Inhibition of rat GAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake by liquid scintillation counting Inhibition of rat GAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake by liquid scintillation counting	[PMID: 25679268]
HEK293	IC₅₀	0.8 μM Compound: (R)-1a	Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis	[PMID: 25882526]
HEK293	IC₅₀	0.8 μM Compound: 1, Tiagabine	Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 3 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells after 3 mins by scintillation counting analysis	[PMID: 23398473]
HEK293	IC₅₀	300 μM Compound: (R)-1a	Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis	[PMID: 25882526]
HEK293	IC₅₀	300 μM Compound: 1, Tiagabine	Inhibition of [3H]GABA uptake at mouse GAT2 expressed in HEK293 cells after 3 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT2 expressed in HEK293 cells after 3 mins by scintillation counting analysis	[PMID: 23398473]
HEK293	IC₅₀	800 μM Compound: (R)-1a	Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis	[PMID: 25882526]
HEK293	IC₅₀	800 μM Compound: 1, Tiagabine	Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK293 cells after 3 mins by scintillation counting analysis Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK293 cells after 3 mins by scintillation counting analysis	[PMID: 23398473]

In Vitro

Tiagabine (0.1-5 μM; 4 days) protects Tet-off PC12 cells expressing mutant huntingtin against toxicity, with significant effects detected at concentrations of 0.5, 2, and 5 μM after 4 days of treatment^[1].
Tiagabine potently and selectively inhibits GABA uptake in glial, neuronal, and synaptosomal preparations, with IC₅₀ values of 0.18 μmol/L, 0.45 μmol/L, and 0.07 μmol/L, respectively^[3].
Tiagabine (2-100 μM; 5-15 min) induces long-lasting, repetitive slow depolarizations in cortical wedges from 20-30 day-old DBA/2 mice, with consistent amplitude and frequency across tested concentrations of 2, 5, 50, and 100 μM following 15-min perfusion, and following shorter 5-10 min perfusions of 50 μM^[4].
Tiagabine (50 μM; 15 min)-induced depolarizations in cortical wedges from 20-30 day-old DBA/2 mice are Ca²⁺-dependent, mediated via GABA_A receptors, require voltage-dependent sodium channel activity, are unaffected by NMDA receptor blockade, are partially inhibited by AMPA receptor blockade, are abolished by Dextromethorphan, and are potentiated by potassium channel blockade^[4].
Tiagabine (50 μM; 15 min) induces depolarizations in cortical wedges from 50 day-old DBAr2 mice and BALB/c mice, similar to responses in 20-30 day-old DBAr2 mice^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay^[1]

Cell Line:

Tet-off PC12 cells expressing mutant huntingtin (htt-N63-148Q)
Concentration:

0.1, 0.5, 1, 2, 5 μM
Incubation Time:

4 days
Result:

Inhibited LDH release induced by mutant htt in a concentration-dependent manner.
Showed statistically significant reductions in LDH release at 0.5, 2, and 5 μM compared to untreated mutant htt-expressing cells.

Parmacokinetics

Species	Dose	Route	Serum Concentration	Brain Concentration
Mice^[1]	5 mg/kg	i.p.	17.2 ± 4.8 ng/mL	177.0 ± 14.2 ng/mL

In Vivo

Tiagabine (2-5 mg/kg; i.p., daily administration, lifelong treatment) extends the survival of male N171-82Q transgenic Huntington's disease mice (up to 33.4 days at the 5 mg/kg dose), improves their motor function, and alleviates brain atrophy and neurodegeneration^[1].
Tiagabine (5 mg/kg; i.p.; daily; lifelong administration) extends the survival of male and female R6/2 transgenic Huntington's disease mice (17.8 days of extension at the dose of 5 mg/kg), improves their motor function, and alleviates brain atrophy^[1].
Tiagabine (0.4 mg/kg; i.p.; single administration; 30 min prior to seizure testing) exerts a protective effect against audiogenic tonic seizures in male DBA/2 mice, with an ED₅₀ of 0.4 mg/kg^[2].
Tiagabine (1.2-1.3 mg/kg; i.p.; single administration; 30 min prior to seizure tests) exerts a protective effect against PTZ-induced tonic convulsions in male NMRI mice, with an ED₅₀ of 1.2 mg/kg, while providing approximately 50% partial protection against clonic convulsions^[2].
Tiagabine (15-30 mg/kg; p.o.; twice daily; for consecutive 21 days) induces tolerance to cognitive effects in mice, but does not induce tolerance to its anticonvulsant effects in DMCM-induced epileptic mice^[3].
Tiagabine (9 mg/kg; subcutaneous injection; once daily for 8 consecutive days; single injection 30 min prior to locomotor activity test) initially reduces short-term spontaneous ethanol intake in ad libitum-fed C57BL/6 mice, but tolerance develops rapidly, resulting in ethanol intake exceeding pre-treatment levels on days 7-8^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

R6/2 mice with Huntington's disease (male, female; CBA/C57Bl6 background; CAG repeat length 110-118; Huntington's disease transgenic model)^[1]
Dosage:

5 mg/kg
Administration:

i.p.; daily; lifelong
Result:

Increased average survival to 102.0 ± 2.9 days compared to 84.2 ± 3.5 days in vehicle controls.
Improved rotarod performance at 10 and 12 weeks of age with statistically significant increases in time on the rod relative to vehicle-treated mice.
Increased striatal volume and reduced lateral ventricle volume relative to vehicle-treated mice, attenuating brain atrophy.
Showed no effect on the number of huntingtin aggregates in the frontal cortex or striatum, and did not affect body weight loss in HD mice.

Animal Model:

C57BL/6 mice with Alcohol use disorder (male, initially 7 weeks old, food-restricted to 80% of ad libitum body weight)^[5]
Dosage:

1 mg/kg; 3 mg/kg; 6 mg/kg; 9 mg/kg
Administration:

s.c.; single injection 30 minutes prior to test; daily for 13 days; single injection 30 minutes prior to post-prandial test
Result:

Produced dose-responsive reductions in lever responses, fountain contacts, and ethanol intake during pre-prandial testing.
Significantly reduced all three measures at 6 mg/kg and 9 mg/kg doses compared to saline.
Reduced lever responses across 13 days of daily 9 mg/kg administration with no evidence of tolerance.
Developed tolerance to the reduction of fountain contacts by the second week of 9 mg/kg daily treatment.
Reduced lever responses at 6 mg/kg, and reduced lever responses, fountain contacts, and ethanol intake at 9 mg/kg during post-prandial testing compared to saline.
Reduced lever responses for ethanol by 43% at 9 mg/kg, a significantly greater reduction than the 26% reduction observed for water.
Reduced motor activity by ~45% on the first day of 9 mg/kg administration, but tolerance to this sedative effect developed by the third daily injection.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 115103-54-3
Appearance Solid
Molecular Weight 375.55
Formel C₂₀H₂₅NO₂S₂
Color Off-white to light yellow
SMILES

O=C([C@H]1CN(CC/C=C(C2=C(C)C=CS2)/C3=C(C)C=CS3)CCC1)O
Synonyms

NO050328; NO328; TGB
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (266.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6628 mL

13.3138 mL

26.6276 mL

5 mM

0.5326 mL

2.6628 mL

5.3255 mL

10 mM

0.2663 mL

1.3314 mL

2.6628 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Masuda N, et al. Tiagabine is neuroprotective in the N171-82Q and R6/2 mouse models of Huntington's disease[J]. Neurobiology of disease, 2008, 30(3): 293-302.

[2]. Nielsen EB, et al. Characterization of tiagabine (NO-328), a new potent and selective GABA uptake inhibitor. Eur J Pharmacol. 1991;196(3):257-266. [Content Brief]

[3]. Adkins J C, et al. Tiagabine: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the management of epilepsy[J]. Drugs, 1998, 55(3): 437-460.

[4]. Hu RQ, et al. Tigabine hydrochloride, an inhibitor of gamma-aminobutyric acid (GABA) uptake, induces cortical depolarizations in vitro. Brain Res. 1997;753(2):260-268. [Content Brief]

[5]. Nguyen SA, et al. Tiagabine reduces ethanol reward in C57BL/6 mice under acute and chronic administration regimens. Synapse. 2005;56(3):135-146. [Content Brief]

[6]. Javaid S, et al. Tiagabine suppresses pentylenetetrazole-induced seizures in mice and improves behavioral and cognitive parameters by modulating BDNF/TrkB expression and neuroinflammatory markers. Biomed Pharmacother. 2023;160:114406. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6628 mL	13.3138 mL	26.6276 mL	66.5690 mL
	5 mM	0.5326 mL	2.6628 mL	5.3255 mL	13.3138 mL
	10 mM	0.2663 mL	1.3314 mL	2.6628 mL	6.6569 mL
	15 mM	0.1775 mL	0.8876 mL	1.7752 mL	4.4379 mL
	20 mM	0.1331 mL	0.6657 mL	1.3314 mL	3.3285 mL
	25 mM	0.1065 mL	0.5326 mL	1.0651 mL	2.6628 mL
	30 mM	0.0888 mL	0.4438 mL	0.8876 mL	2.2190 mL
	40 mM	0.0666 mL	0.3328 mL	0.6657 mL	1.6642 mL
	50 mM	0.0533 mL	0.2663 mL	0.5326 mL	1.3314 mL
	60 mM	0.0444 mL	0.2219 mL	0.4438 mL	1.1095 mL
	80 mM	0.0333 mL	0.1664 mL	0.3328 mL	0.8321 mL
	100 mM	0.0266 mL	0.1331 mL	0.2663 mL	0.6657 mL

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Tiagabine

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Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tiagabine

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

GABA Receptor Compound Library

Human Metabolite Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tiagabine Related Classifications

HY-B0696 Related Classifications