Oxcarbazepine(Synonyms: 奥卡西平; GP 47680)

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Oxcarbazepine (Synonyms: 奥卡西平; GP 47680) 纯度: 98.84%

Oxcarbazepine 是一种钠通道 (sodium channel) 阻滞剂。Oxcarbazepine 有效抑制胶质母细胞瘤细胞生长并诱导胶质母细胞瘤细胞凋亡 (apoptosis) 或 G2/M 停滞。具有抗癌和抗惊厥作用。

Oxcarbazepine(Synonyms: 奥卡西平; GP 47680)

Oxcarbazepine Chemical Structure

CAS No. : 28721-07-5

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10 mM * 1 mL in DMSO ¥610 In-stock
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生物活性

Oxcarbazepine is a sodium channel blocker[1]. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines[2]. Anti-cancer and anticonvulsant effects[2][3].

IC50 & Target

Sodium Channel[1].

体外研究
(In Vitro)

Oxcarbazepine significantly inhibits glioblastoma cell growth and reaches IC50 at therapeutic concentrations. The IC50s of Oxcarbazepine screened with the U87 and T98 cell lines are 12.35 and 9.45 μg/mL,respectively[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.

Cell Viability Assay[2]

Cell Line: Human glioma cell lines U-87 MG and T98G
Concentration: 2.5, 5, 10, 20, and 40 μg/mL
Incubation Time: 72 hours
Result: The growth inhibition for the T98G cell line for each concentration was 17.7±4.1% (2.5 μg/mL), 21.1±3.6% (5 μg/mL), 53.6±14.2% (10 μg/mL), 82.2±2.3% (20 μg/mL), and 85.0±2.3% (40 μg/mL).
The growth inhibition for U-87 MG cell line for each concentration was −1.7±5.1% (0.008 μg/mL), 5.3±2.4% (0.08 μg/mL), 3.5±7.4% (0.8 μg/mL), 0.3±9.2% (16 μg/mL), and −4.2±9.6% (40 μg/mL).

体内研究
(In Vivo)

Oxcarbazepine protectes mice and rats against generalized tonic-clonic seizures induced by electroshock with ED50 values between 13.5 and 20.5 mg/kg p.o. No tolerance toward this anticonvulsant effect is observed when rats are treated with Oxcarbazepine daily for 4 weeks.

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.

Clinical Trial

分子量

252.27

Formula

C15H12N2O2

CAS 号

28721-07-5

中文名称

奥卡西平

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: 

DMSO : 50 mg/mL (198.20 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9640 mL 19.8200 mL 39.6401 mL
5 mM 0.7928 mL 3.9640 mL 7.9280 mL
10 mM 0.3964 mL 1.9820 mL 3.9640 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: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (10.90 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (10.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 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

  • 2.

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

    Solubility: ≥ 2.75 mg/mL (10.90 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (10.90 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 27.5 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]. Ashley M Thomas, et al. Old Friends With New Faces: Are Sodium Channel Blockers the Future of Adjunct Pain Medication Management?J Pain. 2018 Jan;19(1):1-9.

    [2]. Ching-Yi Lee,et al. The effects of antiepileptic drugs on the growth of glioblastoma cell lines. J Neurooncol. 2016 May;127(3):445-53.

    [3]. M Schmutz, et al. Oxcarbazepine: preclinical anticonvulsant profile and putative mechanisms of action. Epilepsia. 1994;35 Suppl 5:S47-50.

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