Tiagabine hydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 4256
Selective GAT-1 inhibitor; anticonvulsant
Key Product Details
Description
Selective GAT-1 inhibitor; anticonvulsant
Product Description
Tiagabine hydrochloride is a GABA uptake inhibitor (IC50 = 67 nM in vivo). Exhibits high affinity and selectivity for the GAT-1 GABA transporter. Anticonvulsant; also attenuates established dynorphin-induced allodynia in a mouse model after systemic administration.Product Specifications
Molecular Weight
412.01
Formula
C20H25NO2S2.HCl
Storage
Desiccate at RT
Purity
≥98% (HPLC)
Chemical Name
(3R)-1-[4,4-Bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid hydrochloride
CAS Number
145821-59-6
PubChem ID
91274
InChI Key
YUKARLAABCGMCN-PKLMIRHRSA-N
SMILES
CC3=C(SC=C3)/C(C2=C(C)C=CS2)=C\CCN1C[C@H](C(O)=O)CCC1.Cl
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 20.6 | 50 | |
| DMSO | 41.2 | 100 |
Preparing Stock Solutions
for Tiagabine hydrochloride
The following data is based on the product molecular weight 412.01
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.43 mL | 12.14 mL | 24.27 mL |
| 5 mM | 0.49 mL | 2.43 mL | 4.85 mL |
| 10 mM | 0.24 mL | 1.21 mL | 2.43 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Dhar Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA updake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. J.Med.Chem. 1994 PMID: 8057281
- Laughlin Comparison of antiepileptic drugs tiagabine, lamotrigine, and gabap. in mouse models of acute, prolonged, and chronic nociception. J.Pharmacol.Exp.Ther. 2002 PMID: 12183677
- Andersen The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug ca J.Med.Chem. 1993 PMID: 8510100
Product Specific Notices for Tiagabine hydrochloride
For research use only
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