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Vigabatrin

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纯度: 99.88%

货号 T0128Cas号 60643-86-9

别名 氨己烯酸, Vigabatrine, Sabril

Vigabatrin (Sabril) 是 γ-氨基丁酸的类似物,是 4-氨基丁酸转氨酶的不可逆抑制剂,负责 γ-氨基丁酸分解代谢。它可用于可卡因依赖的治疗。

Vigabatrin
其他形式的 “Vigabatrin”:

Vigabatrin

一键复制产品信息
Rating icon 很棒

纯度: 99.88%

货号 T0128 别名 氨己烯酸, Vigabatrine, SabrilCas号 60643-86-9

Vigabatrin (Sabril) 是 γ-氨基丁酸的类似物,是 4-氨基丁酸转氨酶的不可逆抑制剂,负责 γ-氨基丁酸分解代谢。它可用于可卡因依赖的治疗。

规格价格库存数量
1 mg
¥ 169
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5 mg
¥ 360
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10 mg
¥ 640
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25 mg
¥ 1,230
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50 mg
¥ 2,120
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100 mg
¥ 3,810
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500 mg
¥ 8,290
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产品介绍


Vigabatrin AI Summary
Vigabatrin exhibits a broad range of bioactivities and pharmacological properties. It demonstrates significant anticonvulsive activity in bicuculline (BIC) and picrotoxin (PCR) induced seizure tests in mice, with effective doses (ED50) of 220.0 umol.kg^-1 and 210.0 umol.kg^-1, respectively. Moreover, at a dosage of 100 mg/kg, it provides sustained protection against picrotoxin-induced convulsions. In terms of metabolism, Vigabatrin has a very short half-life of 0.005 hours at a concentration of 1 mM and a dissociation constant (pKa) of 9.5. It inhibits GABA transaminase (GABA-T) activity in vivo with an IC50 value of 41,210.0 nM and increases brain GABA levels, suggesting potential implications for regulating GABA neurotransmission in the brain. The compound also shows various activities in vitro; it inhibits gamma-aminobutyric acid aminotransferase from the pig brain with a Ki of 3200000.0 nM and a K inact rate of 0.37 min^-1, as well as rat GABA-AT with a Ki of 10,000,000.0 nM. Vigabatrin exhibits inhibitory activity against several human transporters, including BSEP, MRP2, MRP3, and MRP4, with IC50 values greater than 133000.0 nM. While it indicates moderate hepatic toxicity and potential retinotoxicity in specific test conditions, it shows no significant hepatic side effects and good aqueous solubility characteristics. Additionally, Vigabatrin demonstrates significant penetration and inhibition activities related to sodium fluorescein uptake in OATP1B1 and OATP1B3-transfected CHO cells. It has been evaluated for potential antiviral activity against SARS-CoV-2, showing some level of inhibition of virus-induced cytotoxicity and 3CL-Pro protease activity. It also shows a range of potencies in bioactivity assays against various targets, including enzymes and receptors, albeit mostly with high AC50 values, indicating relatively weak interactions. Overall, Vigabatrin has shown potential in modulating GABAergic activity and various other bioactivities, but further investigation is needed to fully understand its pharmacological profile and therapeutic potential..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Vigabatrin (Sabril), an analogue of gamma-aminobutyric acid, is an irreversible inhibitor of 4-aminobutyrate Transaminase responsible for the catabolism of γ-aminobutyric acid.
别名氨己烯酸, Vigabatrine, Sabril
化学信息
分子量129.16
分子式C6H11NO2
CAS No.60643-86-9
SmilesNC(CCC(O)=O)C=C
密度1.108?g/mL?at 25?°C(lit.)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: < 1 mg/mL (insoluble)
H2O: 100 mg/mL (774.23 mM), Sonication is recommended.
溶液配制表
H2O
1mg5mg10mg50mg
1 mM7.7423 mL38.7117 mL77.4234 mL387.1168 mL
5 mM1.5485 mL7.7423 mL15.4847 mL77.4234 mL
10 mM0.7742 mL3.8712 mL7.7423 mL38.7117 mL
20 mM0.3871 mL1.9356 mL3.8712 mL19.3558 mL
50 mM0.1548 mL0.7742 mL1.5485 mL7.7423 mL
100 mM0.0774 mL0.3871 mL0.7742 mL3.8712 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
方案所需的各类助溶剂如: DMSOPEG300PEG400Tween 80SBE-β-CD玉米油等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

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