Stiripentol
(Synonyms: 斯利潘托,BCX2600) 目录号 : GC16951
An antiepileptic compound
Cas No.:49763-96-4
Sample solution is provided at 25 µL, 10mM.
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Stiripentol is an LDH inhibitor. It is a new-generation antiepileptic drug, and its chemical structure is unrelated to other antiepileptic drugs. Seizures and epileptiform activity are reduced by inhibition of the metabolic pathway via lactate dehydrogenase (LDH), which is a component of the astrocyte-neuron lactate shuttle [1].
Stiripentol is used for the treatment of Dravet syndrome, a rare form of epilepsy (26). Stiripentol (300 mg/kg ip) had a small effect on high-voltage spikes in the kainate model. Stiripentol (500 mM) inhibited the lactate-to-pyruvate conversion as well as the pyruvate-to-lactate conversion by both human LDHs. Lineweaver-Burk plots revealed that the inhibition by stiripentol was noncompetitive, suggesting that stiripentol binds to the LDHs at a different site with lactate and pyruvate. [1]
References:
[1]. Sada N, Lee S2, Katsu T et al. Epilepsy treatment. Targeting LDH enzymes with a stiripentol analog to treat epilepsy. Science. 2015 Mar 20;347(6228):1362-7.
| Kinase experiment [1]: | |
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Target |
purified mammalian LDH1 and LDH5 |
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Preparation method |
The solubility of this compound in DMSO is >9.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
500 uM |
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Applications |
Stiripentol inhibited the lactate-to-pyruvate conversion and pyruvate-to-lactate conversion by two human LDHs (LDH1 and LDH5). The inhibition by stiripentol was noncompetitive, suggesting that stiripentol binds to the LDHs at a different site with lactate and pyruvate. |
| Animal experiment [1]: | |
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Animal models |
kainate mice model |
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Dosage form |
300 mg/kg ip |
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Application |
In mice after the kainate injection, stiripentol (300 mg/kg ip) had a small effect on high-voltage spikes. Stiripentol-like compound isosafrole (200 to 300 mg/kg ip) strongly suppressed spontaneous high-voltage spikes and paroxysmal discharges. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Sada N, Lee S2, Katsu T et al. Epilepsy treatment. Targeting LDH enzymes with a stiripentol analog to treat epilepsy. Science. 2015 Mar 20;347(6228):1362-7. | |
| Cas No. | 49763-96-4 | SDF | |
| 别名 | 斯利潘托,BCX2600 | ||
| 化学名 | (E)-1-(benzo[d][1,3]dioxol-5-yl)-4,4-dimethylpent-1-en-3-ol | ||
| Canonical SMILES | OC(C(C)(C)C)/C=C/C1=CC2=C(OCO2)C=C1 | ||
| 分子式 | C14H18O3 | 分子量 | 234.29 |
| 溶解度 | ≥ 9.9mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.2682 mL | 21.3411 mL | 42.6821 mL |
| 5 mM | 0.8536 mL | 4.2682 mL | 8.5364 mL |
| 10 mM | 0.4268 mL | 2.1341 mL | 4.2682 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet