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Isosafrole

现货
Catalog No.
A8703
stiripentol类似物,有效的LDH抑制剂。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,300.00
现货
5mg
¥ 4,500.00
现货
25mg
¥ 12,000.00
现货

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Background

Isosafrole, a stiripentol analog, is a potent LDH inhibitor. Stiripentol 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.
Isosafrole is a substructure of stiripentol that lacks the hydroxyl group and tertiary-butyl group of stiripentol. Isosafrole strongly inhibited the pyruvate-to-lactate conversion by both LDH1 and LDH5, suggesting that it inhibits lactate production itself. Isosafrole (200 to 300 mg/kg ip) strongly suppressed spontaneous high-voltage spikes and paroxysmal discharges in the kainate model in vivo.  Isosafrole suppresses seizures in vivo. Going by the lactate reduction by ketogenic diets, LDH inhibitors for the pyruvate-to-lactate conversion, such as isosafrole, would be more effective for antiepileptic actions.
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 yellow oil
StorageStore at -20°C
M.Wt162.19
Cas No.120-58-1
FormulaC10H10O2
Solubility≥8.8mg/mL in DMSO
Chemical Name(E)-6-(prop-1-en-1-yl)benzo[d][1,3]dioxole
SDFDownload SDF
Canonical SMILESC/C=C/C1=CC=C2C(OCO2)=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

体外实验[1]:

靶点

人LDHs(LDH1和LDH5)

溶解方法

在DMSO中的溶解度>8.8mg/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 μM

应用

Isosafrole强烈抑制LDH1和LDH5引起的丙酮酸向乳酸的转化,表明它本身抑制乳酸生产。

动物实验[1]:

动物模型

红藻氨酸小鼠模型

剂量

100-300 mg/kg; 腹腔注射

应用

在红藻氨酸注射2周后的小鼠海马中,Isosafrole(200-300 mg/kg)强烈地抑制了自发高电压尖峰和阵发性放电。Isosafrole是LDH的抑制剂,可抑制体内癫痫发作。

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.

质量控制

化学结构

Isosafrole