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。
| 生物活性 | Levetiracetam, an antiepileptic agent, binds the synaptic vesicle proteinSV2A. Levetiracetam enhances Temozolomide effect on glioblastoma stem cell proliferation andapoptosis. Levetiracetam modulatesHDAClevels ultimately silencingMGMT, thus increasing Temozolomide effectiveness. A chemosensitizer agent[1][2]. |
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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]
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. |
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体内研究
(In Vivo) | Levetiracetam (10, 25, or 50 mg/kg) suppresses behavioral and electrographic seizure activity during neonatal hypoxia[2].
| 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%. |
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| 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 |
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| 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 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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: ≥ 2.5 mg/mL (14.69 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (14.69 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (14.69 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (14.69 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (14.69 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (14.69 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 25.0 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本网站选购。
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