Stiripentol | Anticonvulsant/LDHA inhibitor

CAS:
 49763-96-4
Catalog Number:
 10-3978
Stiripentol chemical structure

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Stiripentol (49763-96-4) is a clinically useful anticonvulsant used to treat Dravet syndrome.  The precise mechanism of action is unknown but it is thought to act via increasing GABAergic activity1, inhibiting LDHA2 and thereby activating ATP-sensitive potassium channels, and blocking Na+ and Ca2+ channels3. It also inhibits the cytochrome P450 enzymes 1A2, 2C9, 2C19, 2D6, and 3A4.4 Stiripentol and the copper ionophore elesclomol (Cat#10-4238) synergistically suppressed esophageal squamous cell carcinoma (ESCC) tumor growth.2  Lactate dehydrogenase A inhibition by stiripentol reduced ESCC cuproptosis resistance by inhibiting lactylation of NUDT21.

References/CItations:

  1. Quilichini et al. (2006) Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels; Epilepsia, 47 704
  2. Sada et al. (2015) Epilepsy treatment. Targeting LDH enzymes with a stiripentol analog to treat epilepsy; Science, 347 1362
  3. Verleye et al. (2016) Neuroprotective activity of stiripentol with a possible involvement of voltage-dependent calcium and sodium channels; J. Neurosci. Res., 94 179
  4. Tran et al. (1997) Influence of stiripentol on cytochrome P450-mediated metabolic pathways in humans: in vitro and in vivo comparison and calculation of in vivo inhibition constants; Clin. Pharmacol. Ther., 62 490
  5. Lin et al. (2025) NUDT21 lactylation reprograms alternative polyadenylation to promote cuproptosis resistance; Cell Discov., 11 42
49763-96-4, BCX-2600, BCX2600, LDHA inhibitor, NUDT21 lactylation inhibitor, stiripentol, stiripentol and elesclomol, Stiripentol supplier
CAS:
49763-96-4
Catalog Number:
10-3978
Activity:
Anticonvulsant/LDHA inhibitor
Chemical Names:
(E)-1-(1,3-Benzodioxol-5-yl)-4,4-dimethylpent-1-en-3-ol
Alternate Name:
BCX2600
Molecular Weight:
234.30
Molecular Formula:

C14H18O3

Solubility:
Soluble in DMSO (>50 mg/ml)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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Stiripentol (49763-96-4) is a clinically useful anticonvulsant used to treat Dravet syndrome.  The precise mechanism of action is unknown but it is thought to act via increasing GABAergic activity1, inhibiting LDHA2 and thereby activating ATP-sensitive potassium channels, and blocking Na+ and Ca2+ channels3. It also inhibits the cytochrome P450 enzymes 1A2, 2C9, 2C19, 2D6, and 3A4.4 Stiripentol and the copper ionophore elesclomol (Cat#10-4238) synergistically suppressed esophageal squamous cell carcinoma (ESCC) tumor growth.2  Lactate dehydrogenase A inhibition by stiripentol reduced ESCC cuproptosis resistance by inhibiting lactylation of NUDT21.

References/CItations:

  1. Quilichini et al. (2006) Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels; Epilepsia, 47 704
  2. Sada et al. (2015) Epilepsy treatment. Targeting LDH enzymes with a stiripentol analog to treat epilepsy; Science, 347 1362
  3. Verleye et al. (2016) Neuroprotective activity of stiripentol with a possible involvement of voltage-dependent calcium and sodium channels; J. Neurosci. Res., 94 179
  4. Tran et al. (1997) Influence of stiripentol on cytochrome P450-mediated metabolic pathways in humans: in vitro and in vivo comparison and calculation of in vivo inhibition constants; Clin. Pharmacol. Ther., 62 490
  5. Lin et al. (2025) NUDT21 lactylation reprograms alternative polyadenylation to promote cuproptosis resistance; Cell Discov., 11 42

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