Vigabatrin (Synonyms: 氨己烯酸; γ-Vinyl-GABA)
目录号: PL04425 纯度: ≥98%
CAS No. :68506-86-5
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中文名称
Vigabatrin
中文别名
氨己烯酸;4-氨基己-5-烯酸;4-氨基-5-己烯酸;湖北扬信现货供应氨己烯酸杂质ABCDE
英文名称
Vigabatrin
英文别名
Vigabatrin;rac-Vigabatrin DISCONTINUED See V253010;γ-Vinyl-GABA;(±)-γ-Vinyl-GABA;(±)-4-Aminohexenoic acid;(±)-Vigabatrin;(R,S)-4-Amino-5-hexenoic acid
Cas No.
68506-86-5
分子式
C6H11NO2
分子量
129.16
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Vigabatrin (γ-Vinyl-GABA),一种抑制性神经递质 GABA 乙烯基衍生物,是一种具有口服活性且不可逆的 GABA 转氨酶 (GABA transaminase) 抑制剂。 Vigabatrin 是一种抗癫痫剂,通过抑制 GABA transaminase 对 GABA 的分解代谢来增加脑中 GABA 的水平。
生物活性
Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
性状
Solid
体外研究(In Vitro)
A significant increase in seizure threshold is observed following systemic (i.p.) administration of high (600 or 1200 mg/kg) doses of Vigabatrin. Bilateral microinjection of Vigabatrin (10 μg) into either the anterior or posterior substantia nigra pars reticulata (SNr) also increased seizure threshold, but less markedly than systemic treatment. Focal delivery into the subthalamic nucleus (STN) increased seizure threshold more markedly than either intranigral or systemic administration of Vigabatrin. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Vigabatrin inhibits the uptake of taurine in Caco-2 and MDCK cells to 34% and 53%, respectively, at a concentration of 30 mM. In Caco-2 cells the uptake of Vigabatrin under neutral pH conditions is concentration-dependent and saturable with a Km-value of 27 mM. Vigabatrin is able to inhibit the uptake of taurine in intestinal and renal cell culture models. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Broeer, et al. Vigabatrin for focal drug delivery in epilepsy: Bilateral microinfusion into the subthalamic nucleus is more effective than intranigral or systemic administration in a rat seizure model. Neurobiology of Disease (2012), 46(2), 362-376.
[2]. Jakob Plum, et al. The anti-epileptic drug substance vigabatrin inhibits taurine transport in intestinal and renal cell culture models. Int J Pharm. 2014 Oct 1;473(1-2):395-7.
溶解度数据
In Vitro: H2O : 50 mg/mL (387.12 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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