Gabaculine (hydrochloride)
(Synonyms: 格巴库林盐酸盐) 目录号 : GC18336An irreversible inhibitor of GABA-T
Cas No.:59556-17-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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 | |
| 别名 | 格巴库林盐酸盐 | ||
| 化学名 | 5-amino-1,3-cyclohexadiene-1-carboxylic acid, monohydrochloride | ||
| Canonical SMILES | NC1C=CC=C(C(O)=O)C1.Cl | ||
| 分子式 | C7H9NO2.HCl | 分子量 | 175.6 |
| 溶解度 | 0.2mg/mL in ethanol, 20mg/mL in DMSO, 20mg/mL in DMF | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。