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Stiripentol

Catalog No.
A8704
An LDH inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
5mg
$55.00
In stock
10mg
$99.00
In stock
25mg
$220.00
In stock
50mg
$385.00
In stock

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Email: [email protected]

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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
Solubilityinsoluble in H2O; ≥46.7 mg/mL in EtOH; ≥9.9 mg/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
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Kinase experiment [1]:

Target

purified mammalian LDH1 and LDH5

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.

Reacting condition

500 uM

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]:

Animal models

kainate mice model

Dosage form

300 mg/kg ip

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.

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.

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.

Quality Control

Chemical structure

Stiripentol