2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Tiagabine hydrochloride

Tiagabine hydrochloride  (Synonyms: NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride)

Cat. No.: HY-B0696A Purity: 99.44%
COA
SDS
Handling Instructions Technical Support

Tiagabine hydrochloride (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 hydrochloride 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 hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.

For research use only. We do not sell to patients.

Tiagabine hydrochloride

Tiagabine hydrochloride Chemical Structure

CAS No. : 145821-59-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Tiagabine hydrochloride:

Tiagabine hydrochloride Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tiagabine hydrochloride (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 hydrochloride 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 hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease[1][2][3][4][5][6].

IC50 & Target[8]

TrkB

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.049 μM
Compound: 6
Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
[PMID: 23886812]
In Vitro

Tiagabine hydrochloride (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 hydrochloride 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 hydrochloride (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 hydrochloride (50 μM; 15 min)-induced depolarizations in cortical wedges from 20-30 day-old DBA/2 mice are Ca2+-dependent, mediated via GABAA 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 hydrochloride (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.

Tiagabine hydrochloride Related Antibodies
In Vivo

Tiagabine (2-5 mg/kg; i.p., daily administration, lifelong treatment) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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: Tight ligation of L5 and L6 spinal nerves innervating the left hindpaw was performed using aseptic techniques in rats[7]
Dosage: 7.2, 24.3, and 72.8 µmol/kg (3, 10, and 30 mg/kg)
Administration: Intraperitoneal injection (i.p.)
Result: Increased response threshold to tactile stimulation at the highest dose of tiagabine (72.8 µmol/kg) at both 15 and 30 min after injection.
Animal Model: Male mice[7]
Dosage: 0.2, 0.7, 2.4, 7.2, and 24.3 µmol/kg (0.1, 0.3, 1, 3, 10 mg/kg)
Administration: Intraperitoneal injection (i.p.)
Result: Significantly increased foot-licking latency in the hot-plate test at 7.2 and 24.3 µmol/kg.
Significantly increased jump latency at 24.3 µmoles/kg.
Molecular Weight

412.01

Formula

C20H26ClNO2S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (303.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (242.71 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4271 mL 12.1356 mL 24.2713 mL
5 mM 0.4854 mL 2.4271 mL 4.8543 mL
View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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: ≥ 2.08 mg/mL (5.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (5.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.44%

SDS (393 KB)

COA (249 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 2.4271 mL 12.1356 mL 24.2713 mL 60.6781 mL
5 mM 0.4854 mL 2.4271 mL 4.8543 mL 12.1356 mL
10 mM 0.2427 mL 1.2136 mL 2.4271 mL 6.0678 mL
15 mM 0.1618 mL 0.8090 mL 1.6181 mL 4.0452 mL
20 mM 0.1214 mL 0.6068 mL 1.2136 mL 3.0339 mL
25 mM 0.0971 mL 0.4854 mL 0.9709 mL 2.4271 mL
30 mM 0.0809 mL 0.4045 mL 0.8090 mL 2.0226 mL
40 mM 0.0607 mL 0.3034 mL 0.6068 mL 1.5170 mL
50 mM 0.0485 mL 0.2427 mL 0.4854 mL 1.2136 mL
60 mM 0.0405 mL 0.2023 mL 0.4045 mL 1.0113 mL
80 mM 0.0303 mL 0.1517 mL 0.3034 mL 0.7585 mL
100 mM 0.0243 mL 0.1214 mL 0.2427 mL 0.6068 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Tiagabine hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tiagabine145821-59-6NO050328NO328TGBNO 050328NO-050328NO 328NO-328GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorPC12NeuroprotectiveR6/2NeuroinflammatoryAnti-allodynicAntinociceptivePD.Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Tiagabine hydrochloride
Cat. No.:
HY-B0696A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.