GlpBio

Vigabatrin

目录号: GC37905纯度: >98.00%同义词: 氨己烯酸; γ-Vinyl-GABA
Vigabatrin是 γ-氨基丁酸转氨酶 (GABA-T) 的不可逆抑制剂，具有提高脑 GABA 水平和增强抑制性神经传递的强效活性。
Vigabatrin
Cas No.: 68506-86-5
规格价格库存数量操作
5mg¥350.00现货
1
10mg¥560.00现货
1
50mg¥2,240.00现货
1
10mM (in 1mL Water)¥616.00现货
1
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产品描述 Description

Vigabatrin is an irreversible inhibitor of γ-aminobutyric acid transaminase (GABA-T), with potent activity in elevating brain GABA levels and enhancing inhibitory neurotransmission [1-3]. Vigabatrin is commonly used to treat refractory epilepsy [4].

In glioblastoma multiforme cell (13–06-MG), concentration-dependent inhibitory effect of Vigabatrin (0.3-100μM; 24h) on the activity of IKCa channels [5]. In Caco-2 and MDCK cells, Vigabatrin (30mM; 24h) inhibits the uptake of taurine in Caco-2 and MDCK cells to 34 ± 3 and 53 ± 2% [6]. In U87 cells, Vigabatrin administration has a growth-promoting effect on cells [7].

In Tsc1GFAPCKO mice, Vigabatrin (50mg/kg, 100mg/kg, 200mg/kg; ip; 10 weeks) treatment decreased the development of seizures and modestly improved survival [8]. In C57BL/6J mice, after of Vigabatrin (140mg/kg; ip; 4 weeks) treatment, ERG b-wave amplitude was enhanced, and amplitudes of oscillatory potentials were reduced [9]. In C57BL/6J mice, Vigabatrin (35-140mg/kg; sc; 14d) treatment induces amino acid disturbances in mice [10].

References:
[1]. French JA. Vigabatrin. Epilepsia. 1999 May; 40: s11-6.
[2]. James Willmore L, Abelson MB, Ben‐Menachem E, et al. Vigabatrin: 2008 update. Epilepsia. 2009 Feb; 50(2): 163-173.
[3]. Ben‐Menachem E. Mechanism of action of vigabatrin: correcting misperceptions. Acta neurologica scandinavica. 2011 Dec; 124: 5-15.
[4]. Tartara A, Manni R, Galimberti CA, et al. Vigabatrin in the treatment of epilepsy: a double‐blind, placebo‐controlled study. Epilepsia. 1986 Dec; 27(6): 717-723.
[5]. Hung TY, Huang HY, Wu SN, et al. Depressive effectiveness of vigabatrin (γ-vinyl-GABA), an antiepileptic drug, in intermediate-conductance calcium-activated potassium channels in human glioma cells. BMC Pharmacology and Toxicology. 2021 Dec; 22: 1-9.
[6]. Plum J, Nøhr MK, Hansen SH, et al. The anti-epileptic drug substance vigabatrin inhibits taurine transport in intestinal and renal cell culture models. International journal of pharmaceutics. 2014 Oct 1; 473(1-2): 395-397.
[7]. Lee CY, Lai HY, Chiu A, et al. The effects of antiepileptic drugs on the growth of glioblastoma cell lines. Journal of neuro-oncology. 2016 May; 127: 445-453.
[8]. Zhang B, McDaniel SS, Rensing NR, et al. Vigabatrin inhibits seizures and mTOR pathway activation in a mouse model of tuberous sclerosis complex. PLoS One. 2013 Feb 20; 8(2): e57445.
[9]. Chan K, Hoon M, Pattnaik BR, et al. Vigabatrin-induced retinal functional alterations and second-order neuron plasticity in C57BL/6J mice. Investigative Ophthalmology & Visual Science. 2020 Feb 7; 61(2): 17.
[10]. Walters DC, Arning E, Bottiglieri T, et al. Metabolomic analyses of vigabatrin (VGB)-treated mice: GABA-transaminase inhibition significantly alters amino acid profiles in murine neural and non-neural tissues. Neurochemistry international. 2019 May 1; 125: 151-162.

Vigabatrin是 γ-氨基丁酸转氨酶 (GABA-T) 的不可逆抑制剂，具有提高脑 GABA 水平和增强抑制性神经传递的强效活性 [1-3]。Vigabatrin常用于治疗难治性癫痫 [4]。

在多形性胶质母细胞瘤细胞（13-06-MG）中，Vigabatrin（0.3-100μM；24h）对IKCa通道活性具有浓度依赖性的抑制作用 [5]。在Caco-2和MDCK细胞中，Vigabatrin（30mM；24h）可抑制Caco-2和MDCK细胞对牛磺酸的摄取，使其分别降低34±3%和53±2% [6]。在U87细胞中，Vigabatrin给药促进细胞生长的作用 [7]。

在Tsc1GFAPCKO小鼠中，Vigabatrin（50mg/kg、100mg/kg、200mg/kg；ip；10周）治疗可减少癫痫发作，并略微提高生存率 [8]。在C57BL/6J小鼠中，Vigabatrin（140mg/kg；ip；4周）治疗后，ERG b波幅度增强，振荡电位幅度降低 [9]。在C57BL/6J小鼠中，Vigabatrin（35-140mg/kg；sc；14d）治疗可诱发小鼠氨基酸紊乱 [10]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Glioblastoma multiforme cell (13–06-MG)

Preparation Method

The glioblastoma multiforme cell (13–06-MG) were cultured at a density of 106/mL in high glucose (4g/L) Dulbecco’s modified Eagle media supplemented with 10% heat-inactivated fetal bovine serum, 100 U/mL penicillin and 10μg/mL streptomycin. Cells were maintained at 37 ℃ in a 5% CO2 incubator as monolayer cultures and thereafter sub-cultured weekly. Fresh media was added every 2–3 days in order to ensure a healthy cell population. To evaluate concentration-dependent inhibition of VGB on the probability of IKCa channels that would be open, we kept 13–06-MG cells to be bathed in normal Tyrode’s solution containing 1.8mM CaCl2, and each cell examined was voltage-clamped at -80mV relative to the bath. The probability of channel opening was measured in the control or during cell exposure to different concentrations (0.3-100μM) of Vigabatrin; and, these values were then compared with those taken after the addition of TRAM-34 (3μM). TRAM-34 is a known selective blocker of IKCa channels.

Reaction Conditions

0.3-100μM; 24h

Applications

Concentration-dependent inhibitory effect of Vigabatrin on the activity of IKCa channels.

Animal experiment [2]:

Animal models

Tsc1GFAPCKO mice

Preparation Method

Three-week-old Tsc1GFAPCKO mice were treated with vehicle (saline) or Vigabatrin at different doses (50, 100, 200mg/kg/day, i.p) for one week for Western blot and GABA concentrations, for four weeks (200mg/kg/day) for histology and immunohistochemistry analysis, and for up to 10 weeks (200mg/kg/day) for video-EEG monitoring.

Dosage form

50mg/kg, 100mg/kg, 200mg/kg; ip; 10 weeks

Applications

Vigabatrin treatment decreased the development of seizures and modestly improved survival in Tsc1GFAPCKO mice.

References:
[1]. Hung TY, Huang HY, Wu SN, et al. Depressive effectiveness of vigabatrin (?-vinyl-GABA), an antiepileptic drug, in intermediate-conductance calcium-activated potassium channels in human glioma cells. BMC Pharmacology and Toxicology. 2021 Dec; 22: 1-9.
[2]. Zhang B, McDaniel SS, Rensing NR, et al. Vigabatrin inhibits seizures and mTOR pathway activation in a mouse model of tuberous sclerosis complex. PLoS One. 2013 Feb 20; 8(2): e57445.

产品文档 Product Documents

Purity:>98.00%Appearance:A solid

化学性质Chemical Properties

CAS 号
68506-86-5
同义词
氨己烯酸; γ-Vinyl-GABA
化学名
4-amino-5-hexenoic acid
SMILES
C=CC(N)CCC(O)=O
分子式
C6H11NO2
分子量
129.16 g/mol
溶解性
10mg/mL in PBS, pH 7.2
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

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