Levetiracetam(Synonyms: 左乙拉西坦; UCB L059)

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Levetiracetam (Synonyms: 左乙拉西坦; UCB L059) 纯度: 99.99%

Levetiracetam是一种抗癫痫药,结合突触小泡蛋白 SV2A。 Levetiracetam增强Temozolomide 对胶质母细胞瘤干细胞增殖和凋亡的影响。Levetiracetam调节 HDAC 水平,最终使 MGMT 沉默从而提高 Temozolomide的有效性。化学增敏剂。

Levetiracetam(Synonyms: 左乙拉西坦; UCB L059)

Levetiracetam Chemical Structure

CAS No. : 102767-28-2

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10 mM * 1 mL in DMSO ¥768 In-stock
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生物活性

Levetiracetam, an antiepileptic agent, binds the synaptic vesicle protein SV2A. Levetiracetam enhances Temozolomide effect on glioblastoma stem cell proliferation and apoptosis. Levetiracetam modulates HDAC levels ultimately silencing MGMT, thus increasing Temozolomide effectiveness. A chemosensitizer agent[1][2].

IC50 & Target

M2 mAChR[1]

体外研究
(In Vitro)

Levetiracetam increases the transcription of HDACs and recruits corepressor complex on O6-Methylguanine-DNA-methyltransferase (MGMT) promoter, thus silencing its activity[1].
Levetiracetam sensitizes (40 μg/mL) glioblastoma multiforme stem-like cells (GSCs) to Temozolomide (250 µM) treatment[1].
MGMT expression is downregulated in GCSCs treated with Levetiracetam (40 μg/mL)[1]

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: GCSC neurospheres
Concentration: 40 μg/mL
Incubation Time: 48 hours
Result: Slight antitumor effect exerted by the treatment with Temozolomide (250 µM) or Levetiracetam (40 μg/mL) alone was strongly enhanced when Temozolomide and Levetiracetam were added in combination.

Western Blot Analysis[1]

Cell Line: Glioblastoma multiforme stem-like cells (GSCs)
Concentration: 40 μg/mL
Incubation Time: 48 hours
Result: A high level of MGMT expression in untreated GCSCs; this expression was slightly decreased after treatment with Temozolomide (250 µM) and Levetiracetam singularly but it was dramatically decreased after the combined treatment with Temozolomide and Levetiracetam.

体内研究
(In Vivo)

Levetiracetam (10, 25, or 50 mg/kg) suppresses behavioral and electrographic seizure activity during neonatal hypoxia[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Long-Evans rats[2]
Dosage: 10, 25, or 50 mg/kg
Administration: Intraperitoneal injection 60 min before hypoxia.
Result: Treatment resulted in a significant decrease in hypoxic seizure (HS) duration at 25 mg/kg and at 50 mg/kg. Anticonvulsant activity was maximal at 50 mg/kg, at which HSs were reduced by 63.6%.

Clinical Trial

分子量

170.21

Formula

C8H14N2O2

CAS 号

102767-28-2

中文名称

左乙拉西坦;乐凡替拉西坦;利维西坦;左旋乙拉西坦

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : ≥ 85 mg/mL (499.38 mM)

DMSO : ≥ 85 mg/mL (499.38 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.8751 mL 29.3755 mL 58.7510 mL
5 mM 1.1750 mL 5.8751 mL 11.7502 mL
10 mM 0.5875 mL 2.9375 mL 5.8751 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (587.51 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (12.75 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (12.75 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (12.75 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (12.75 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (12.75 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (12.75 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Bianca Maria Scicchitano, et al. Levetiracetam enhances the temozolomide effect on glioblastoma stem cell proliferation and apoptosis. Cancer Cell Int. 2018 Sep 10;18:136.

    [2]. Delia M Talos, et al. Antiepileptic effects of levetiracetam in a rodent neonatal seizure model. Pediatr Res. 2013 Jan;73(1):24-30.

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