Stiripentol (Synonyms: BCX 2600) |
| Katalog-Nr.GC16951 |
Stiripentol (STP) ist ein Antikonvulsivum, das die durch CYP3A4 (nicht kompetitiv) und CYP2C19 (kompetitiv) vermittelte N-Demethylierung von CLB zu NCLB mit Ki von 1,59 ± 0,07 und 0,516 ± 0,065 μM und IC50 von 1,58 bzw. 3,29 μM hemmen kann .
Products are for research use only. Not for human use. We do not sell to patients.
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.
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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