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Stiripentol

Catalog No.
A8704
LDH抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
5mg
¥ 530.00
现货
10mg
¥ 840.00
现货
25mg
¥ 1,520.00
现货
50mg
¥ 2,090.00
现货

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Background

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.

Chemical Properties

Physical AppearanceA colorless liquid
StorageStore at -20°C
M.Wt234.29
Cas No.49763-96-4
FormulaC14H18O3
Solubility≥9.9mg/mL in DMSO
Chemical Name(E)-1-(benzo[d][1,3]dioxol-5-yl)-4,4-dimethylpent-1-en-3-ol
SDFDownload SDF
Canonical SMILESOC(C(C)(C)C)/C=C/C1=CC2=C(OCO2)C=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验[1]:

靶点

纯化的哺乳动物LDH1和LDH5

溶解方法

在DMSO中的溶解度>9.9mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

500 uM

应用

Stiripentol抑制两种人类LDH(LDH1和LDH5)诱导的乳酸 - 丙酮酸转化和丙酮酸 - 乳酸转化。Stiripentol的抑制是非竞争性的,表明Stiripentol与乳酸和丙酮酸在不同部位与LDHs结合。

动物实验[1]:

动物模型

红藻氨酸小鼠模型

剂量

300 mg/kg,腹腔注射

应用

在红藻氨酸注射后的小鼠中,stiripentol(300mg / kg ip)对高电压峰值影响很小。Stiripentol样化合物isosafrole(200-300 mg / kg ip)强烈抑制自发性高电压尖峰和阵发性放电。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

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.

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