Gabaculine (hydrochloride) |
| رقم الكتالوجGC18336 |
An irreversible inhibitor of GABA-T
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 59556-17-1
Sample solution is provided at 25 µL, 10mM.
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Gabaculine is a naturally occurring, conformationally constrained analog of GABA and an irreversible inhibitor of GABA transaminase (GABA-T; Ki = 2.9 μM). [1] It irreversibly inhibits D-amino acid transaminase, L-alanine transaminase, and L-aspartate transaminase with Ki values of 0.1, 1, and 55 mM, respectively.[2] Gabaculine also irreversibly inhibits ornithine aminotransferase in vitro and in mouse brain and liver homogenates, where ornithine aminotransferase activity is suppressed for over 24 hours when administered at a dose of 50 mg/kg. [3] Gabaculine increases latency to convulsion in the 3-mercaptopropionic acid-induced and minimal electroshock-induced seizure models (ED50s = 135 and 200 mg/kg, respectively) and inhibits 3-mercaptopropionic acid-induced increases in glutamic acid decarboxylase (GAD) activity and GABA-T activity in mice (ED50s =135 mg/kg), however, the doses fall above the LD50 value of 62 mg/kg. [4] Gabaculine (135 mg/kg, i.p.) elevates concentrations of GABA in mouse brain by over 500% and knocks out GABA-T activity to below detection limits.
Reference:
[1]. Rando, R.R. Mechanism of the irreversible inhibition of γ-aminobutyric acid--ketoglutaric acid transaminase by the neurotoxin gabaculine. Biochem J. 16(21), 4604-4610 (1977).
[2]. Soper, T.S., and Manning, J.M. Inactivation of pyridoxal phosphate enzymes by gabaculine. Correlation with enzymic exchange of β-protons. J. Biol. Chem. 257(23), 13930-13936 (1982).
[3]. Jung, M.J., and Seiler, N. Enzyme-activated irreversible inhibitors of L-ornithine:2-oxoacid aminotransferase. Demonstration of mechanistic features of the inhibition of ornithine aminotransferase by 4-aminohex-5-ynoic acid and gabaculine and correlation with in vivo activity. J. Biol. Chem. 253(20), 7431-7439 (1978).
[4]. Löscher, W. 3-Mercaptopropionic acid: convulsant properties, effects on enzymes of the γ-aminobutyrate system in mouse brain and antagonism by certain anticonvulsant drugs, aminooxyacetic acid and gabaculine. Biochem. Pharmacol. 28(8), 1397-1407 (1979).
| Cas No. | 59556-17-1 | SDF | |
| Chemical Name | 5-amino-1,3-cyclohexadiene-1-carboxylic acid, monohydrochloride | ||
| Canonical SMILES | NC1C=CC=C(C(O)=O)C1.Cl | ||
| Formula | C7H9NO2.HCl | M.Wt | 175.6 |
| الذوبان | 0.2mg/mL in ethanol, 20mg/mL in DMSO, 20mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.6948 mL | 28.4738 mL | 56.9476 mL |
| 5 mM | 1.139 mL | 5.6948 mL | 11.3895 mL |
| 10 mM | 0.5695 mL | 2.8474 mL | 5.6948 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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