| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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Tiagabine HCl (NNC-05-0328; NO-05-0328; NO329; NNC-050328; NO 329; trade name Gabitril), the hydrochloride salt of tiagabine, is an marketed anticonvulsant acting as a selective GABA (gamma-aminobutyric acid) reuptake inhibitor, may also be used for the treatment of panic disorders.
| References |
:Cochrane Database Syst Rev. 2012 Dec 12;12:CD004694. |
|---|---|
| Additional Infomation |
Tiagabine hydrochloride is a hydrochloride resulting from the reaction of equimolar amounts of tiagabine and hydrogen chloride. A GABA reuptake inhibitor, it is used for the treatment of epilepsy. It has a role as an anticonvulsant and a GABA reuptake inhibitor. It contains a tiagabine(1+).
Tiagabine Hydrochloride is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. Tiagabine hydrochloride inhibits the gamma-aminobutyric acid (GABA) transporter type 1 (GAT1), which is predominantly localized in presynaptic terminals of neurons thereby preventing the reuptake of GABA by the presynaptic endings. Consequently, this increases the level of available GABA within the synaptic cleft, thereby resulting in prolongation of its inhibitory actions. Tiagabine is effective against maximum electroshock seizures and both limbic and generalized tonic-clonic seizures. A nipecotic acid derivative that acts as a GABA uptake inhibitor and anticonvulsant agent. It is used in the treatment of EPILEPSY, for refractory PARTIAL SEIZURES. See also: Tiagabine (has active moiety). |
| Molecular Formula |
C20H26CLNO2S2
|
|---|---|
| Molecular Weight |
412.003
|
| Exact Mass |
411.109
|
| CAS # |
145821-59-6
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| Related CAS # |
Tiagabine;115103-54-3;Tiagabine hydrochloride hydrate;145821-57-4
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| PubChem CID |
91274
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| Appearance |
White to off-white solid powder
|
| Boiling Point |
568ºC at 760 mmHg
|
| Melting Point |
>192oC dec.
|
| Flash Point |
297.3ºC
|
| Vapour Pressure |
9.71E-14mmHg at 25°C
|
| LogP |
5.784
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
26
|
| Complexity |
474
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC1=C(SC=C1)C(=CCCN2CCC[C@H](C2)C(=O)O)C3=C(C=CS3)C.Cl
|
| InChi Key |
YUKARLAABCGMCN-PKLMIRHRSA-N
|
| InChi Code |
InChI=1S/C20H25NO2S2.ClH/c1-14-7-11-24-18(14)17(19-15(2)8-12-25-19)6-4-10-21-9-3-5-16(13-21)20(22)23;/h6-8,11-12,16H,3-5,9-10,13H2,1-2H3,(H,22,23);1H/t16-;/m1./s1
|
| Chemical Name |
(R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl)piperidine-3-carboxylic acid hydrochloride
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| Synonyms |
NNC-05-0328; NO-05-0328; NO329; NNC-050328; NO 329; trade name Gabitril
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~242.71 mM)
DMSO : ≥ 53 mg/mL (~128.64 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4272 mL | 12.1359 mL | 24.2718 mL | |
| 5 mM | 0.4854 mL | 2.4272 mL | 4.8544 mL | |
| 10 mM | 0.2427 mL | 1.2136 mL | 2.4272 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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