| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Gabaculine HCl targets GABA transaminase (GABA-T), the enzyme responsible for the catabolism of the inhibitory neurotransmitter GABA. By inhibiting GABA-T, gabaculine prevents the breakdown of GABA, leading to increased GABA levels in the synaptic cleft. This enhances GABAergic neurotransmission, resulting in increased inhibitory signaling in the brain. The compound's mechanism is similar to that of other GABA-T inhibitors, such as vigabatrin. It is a potent and irreversible inhibitor of GABA-T.
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| ln Vitro |
In vitro, gabaculine HCl is a potent inhibitor of GABA transaminase activity. Its inhibitory activity has been characterized in enzymatic assays using purified GABA-T preparations. The compound irreversibly binds to the enzyme, leading to sustained inhibition. Its effects on GABA levels have been demonstrated in various in vitro systems. Its potency and selectivity for GABA-T have been established.
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| ln Vivo |
In vivo, gabaculine HCl increases GABA levels in the brain by inhibiting GABA-T. This leads to enhanced GABAergic neurotransmission and increased inhibitory signaling. The compound has been used in animal models to study the role of GABA in various neurological and psychiatric disorders. Its effects on behavior, seizure activity, and neurotransmitter levels have been studied. Specific dosing regimens are available in the scientific literature.
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| Enzyme Assay |
In vitro enzyme assays for gabaculine HCl involve measuring the inhibition of GABA transaminase activity using purified enzyme preparations. The compound is incubated with GABA-T and its substrate GABA, and the production of succinic semialdehyde is measured using spectrophotometric or chromatographic methods. The IC50 value is determined from dose-response curves. The compound's irreversible binding can be confirmed by dialysis experiments.
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| Cell Assay |
In vitro cell-based assays for gabaculine HCl involve treating neuronal cells with the compound to assess its effects on GABA levels and GABAergic signaling. GABA levels in cell lysates or culture media are measured using HPLC or ELISA. The compound's effects on neuronal activity can be assessed using electrophysiological recordings. These assays characterize the compound's cellular activity.
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| Animal Protocol |
In vivo animal experiments for gabaculine HCl have been conducted in models of epilepsy, anxiety, and other neurological disorders. The compound is typically administered via injection. Its effects on seizure activity, anxiety-like behavior, and GABA levels in the brain are assessed. Efficacy endpoints depend on the specific model being studied. These studies have helped elucidate the role of GABA in various neurological conditions.
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| ADME/Pharmacokinetics |
Gabaculine HCl has a molecular weight of 168.62 and a molecular formula of C6H9ClN2O2. It is a hydrochloride salt of gabaculine. The compound is a naturally occurring amino acid analog. It is typically dissolved in water or saline for in vivo administration. Its pharmacokinetic properties, including brain penetration, have been characterized in preclinical studies. It is typically stored under recommended conditions for research compounds.
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| Toxicity/Toxicokinetics |
Specific toxicity data for gabaculine HCl is not extensively reported. As a GABA-T inhibitor, its safety profile is related to its effects on GABAergic neurotransmission. The compound may cause sedation, ataxia, and other CNS effects at high doses. Comprehensive toxicological studies would be required for therapeutic development. Standard safety precautions should be taken when handling the compound.
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| References | |
| Additional Infomation |
Gabaculine HCl is a potent inhibitor of GABA transaminase (GABA-T) used in research to study GABAergic neurotransmission. It is a naturally occurring amino acid analog. By inhibiting GABA-T, gabaculine increases GABA levels in the brain. The compound has been used in animal models to study epilepsy, anxiety, and other neurological disorders. Gabaculine HCl is a research tool for studying the role of GABA in the brain.
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| Molecular Formula |
C7H9NO2.HCL
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|---|---|
| Molecular Weight |
175.6128
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| Exact Mass |
175.04
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| CAS # |
59556-17-1
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| Related CAS # |
59556-29-5;59556-17-1 (HCl);
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| PubChem CID |
198382
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| Appearance |
White to off-white solid powder
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| Boiling Point |
304.6ºC at 760 mmHg
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| Melting Point |
203ºC (dec.)(lit.)
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| Flash Point |
138ºC
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| LogP |
1.786
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
11
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| Complexity |
206
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OBZFLUDUSNCZKL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H9NO2.ClH/c8-6-3-1-2-5(4-6)7(9)10;/h1-3,6H,4,8H2,(H,9,10);1H
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| Chemical Name |
5-aminocyclohexa-1,3-diene-1-carboxylic acid;hydrochloride
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| 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.6944 mL | 28.4722 mL | 56.9444 mL | |
| 5 mM | 1.1389 mL | 5.6944 mL | 11.3889 mL | |
| 10 mM | 0.5694 mL | 2.8472 mL | 5.6944 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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