2. Membrane Transporter/Ion Channel Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. GABA Receptor Trk Receptor
  4. Tiagabine hydrochloride

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

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

Tiagabine hydrochloride is an anticonvulsant agent and a selective inhibitor of the GAT-1 GABA transporter with a Ki of ∼0.1 μM. Tiagabine hydrochloride potently and selectively inhibits GABA reuptake with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in synaptosomes, neurons and glia, respectively. Tiagabine hydrochloride has neuroprotective properties.

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Tiagabine hydrochloride Chemical Structure

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
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Based on 1 publication(s) in Google Scholar

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Tiagabine hydrochloride Related Antibodies

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Description

Tiagabine hydrochloride is an anticonvulsant agent and a selective inhibitor of the GAT-1 GABA transporter with a Ki of ∼0.1 μM. Tiagabine hydrochloride potently and selectively inhibits GABA reuptake with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in synaptosomes, neurons and glia, respectively. Tiagabine hydrochloride has neuroprotective properties[1][2][3][4][5][6][7][8].

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 (0.1 μM) hydrochloride inhibits GABA uptake in temporal cortex and white structures from pig brain (50% and 60–68%, respectively)[2].
Tiagabine (0.1-5 μM) protects neurons against mutant huntingtin (htt)-induced toxicity (withdrawal of Doxycycline (HY-N0565)) in PC12 cells[4].
Tiagabine (20-100 μM, 1 h) increases viability of SH-SY5Y cells treated with 1 mM MPP+[5].
Tiagabine (25 min) inhibits [3H]GABA uptake at mouse GAT1 expressed in HEK293 cells, with IC50 of 0.07 μM[6].

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

Tiagabine hydrochloride Related Antibodies
In Vivo

Tiagabine hydrochloride (2-5 mg/kg, i.p., daily) is neuroprotective in the N171-82Q and R6/2 mouse models of Huntington's disease, with improving motor performance and attenuating brain atrophy and neurodegeneration[4].
Tiagabine hydrochloride (5 mg/kg, i.p.) acts as a brake for nigrostriatal microglial activation and reduces dopaminergic neuronal loss in MPTP- and LPS-induced models of PD mice[5].
Tiagabine hydrochloride shows dose-dependent anti-allodynic effect in a rat model of neuropathic pain (3-30 mg/kg, i.p.) and antinociceptive effects against acute thermal pain in mice (in hot-plate test, 3-10 mg/kg, i.p.)[7].
Tiagabine (0.5-2 mg/kg, i.p., 21 days) hydrochloride suppresses pentylenetetrazole-induced seizures in mice and improves behavioral and cognitive parameters by modulating BDNF/TrkB expression and neuroinflammatory markers[8].

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.
Clinical Trial
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: 

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

DMSO : ≥ 53 mg/mL (128.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

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
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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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
DMSO / H2O 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.

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Tiagabine hydrochloride Related Classifications

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  • 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 ReceptorTrk ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorTropomyosin related kinase receptorPC12NeuroprotectiveR6/2NeuroinflammatoryAnti-allodynicAntinociceptivePD.Inhibitorinhibitorinhibit

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