Stiripentol
Based on 7 publication(s) in Google Scholar
Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.99%
- No. CAS: 49763-96-4
- Fòrmula: C14H18O3
- Peso molecular:234.29
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Stiripentol
More
Customer Validation & Images
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Cell Migration/Invasion Assay
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RT-PCR
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WB
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In Vivo Efficacy Study
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RT-PCR
Actividad biológica
Descripciòn
IC50 & Target
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CYP2 |
CYP3 |
In Vitro
Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to N-desmethylclobazam (NCLB) mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively). The inhibition of CLB demethylation by Stiripentol (STP) is best described by a noncompetitive inhibition model with apparent Ki=1.6 μM for the cDNA-expressing CYP3A4 and by a competitive inhibition model with Ki=0.52 μM for the cDNA-expressing CYP2C19. Formation of OH-NCLB from NCLB by cDNA-expressing CYP2C19 is competitively inhibited by Stiripentol (STP) with a Ki=0.14 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 49763-96-4
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Appearance Solid
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Peso molecular 234.29
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Fòrmula C14H18O3
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Color White to off-white
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SMILES
CC(C)(C)C(O)/C=C/C1=CC=C(OCO2)C2=C1
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Synonyms
BCX2600
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
Lactate dehydrogenase A regulates tumor-macrophage symbiosis to promote glioblastoma progression. [Abstract]2024 Mar 5;15(1):1987. PMID: 38443336
Stiripentol purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Mar 5;15(1):1987. [Abstract]
Stiripentol (5 μM) inhibited CT2A CM-induced migration of Raw264.7 macrophages.
Stiripentol purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Mar 5;15(1):1987. [Abstract]
Stiripentol (10 μM) reduced CCL2 expression in human GSC272 cells.
Stiripentol purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Mar 5;15(1):1987. [Abstract]
Stiripentol (10 μM) reduced CCL7 expression in human GSC272 cells.
Stiripentol purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Mar 5;15(1):1987. [Abstract]
Stiripentol (150 mg/kg, i.p., every other day for 6 doses) inhibited tumor growth and prolonged survival in C57BL/6 mice implanted with CT2A cells, GL261 cells, and 005 GSCs.
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J Clin Invest
Symbiotic exclusivity between CLOCK and TFPI2 drives stemness and immunosuppression in glioblastoma models. [Abstract]2026 Mar 17:e199056. PMID: 41842961 -
Adv Sci (Weinh)
Histone H3K9 Lactylation Confers Temozolomide Resistance in Glioblastoma via LUC7L2-Mediated MLH1 Intron Retention. [Abstract]2024 May;11(19):e2309290. PMID: 38477507
Stiripentol purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 May;11(19):e2309290. [Abstract]
Stiripentol (500 µM) significantly reduced the mRNA expression level of LUC7L2 in TBD0220TR cells.
Stiripentol purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 May;11(19):e2309290. [Abstract]
Stiripentol (500 µM) significantly reduced the protein expression level of LUC7L2 in TBD0220TR cells.
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PNAS Nexus
Oncogenic PIK3CA mutations shape an immunoregulatory microenvironment in mosaic overgrowth disorders. [Abstract]2026 May 13;5(6):pgag163. PMID: 42222744 -
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Res Sq
2023 Oct 5:rs.3.rs-3401154. PMID: 37886538
Solvente y solubilidad
In Vitro:
DMSO : 150 mg/mL (640.23 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (8.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 25 mg/mL (106.71 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Cell Assay[1]
The inhibition constants (apparent Ki) of Stiripentol (STP) for CLB demethylation by CYP3A4 and CYP2C19 are determined using various concentrations of CLB (2, 10, 20, 40, 60, and 100 μM) with increasing concentrations of Stiripentol (STP) (0, 0.5, 1, 2, and 5 μM). Concerning NCLB hydroxylation by CYP2C19, the apparent Ki is similarly determined with different concentrations of NCLB (1.5, 4, 6, 8, 12, and 14 μM) and STP (0, 0.1, 0.5, 1, and 2 μM). IC50 values are determined by coincubation of the substrate at concentration in the range of the therapeutic plasma concentrations (2 μM CLB or 14 μM NCLB) with increasing concentrations of Stiripentol (STP) (0.001, 0.002, 0.005, 0.01, 0.05, 0.1, 0.25, 2, 5, and 10 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[2]
Two age groups, p1M (n=18, age 4 weeks) and p5M (n=18, age 5-10 months), of Scn1aRX/+ mice are assigned in this experiment. Both groups are divided randomly into three subgroups (n=6), and each subgroup is administered Stiripentol (STP) (300 mg/kg) alone, CLB (6.62 mg/kg) alone, or a combination of Stiripentol (STP) (p1M; 150 mg/kg, p5M; 300 mg/kg) and CLB (6.62 mg/kg). All drugs are administered by intraperitoneal injection (i.p.) after a 48-h recovery from baseline seizure study. Blood samples are collected at 1 h and 20 min after administration of CLB or STP+CLB for measurement of plasma concentrations of CLB and N-desmethylclobazam, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Giraud C, et al. In vitro and in vivo inhibitory effect of stiripentol on clobazam metabolism.Drug Metab Dispos. 2006 Apr;34(4):608-11. Epub 2006 Jan 13. [Content Brief]
[2]. Cao D, et al. Efficacy of stiripentol in hyperthermia-induced seizures in a mouse model of Dravet syndrome. Epilepsia. 2012 Jul;53(7):1140-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.2682 mL | 21.3411 mL | 42.6821 mL | 106.7054 mL |
| 5 mM | 0.8536 mL | 4.2682 mL | 8.5364 mL | 21.3411 mL | |
| 10 mM | 0.4268 mL | 2.1341 mL | 4.2682 mL | 10.6705 mL | |
| 15 mM | 0.2845 mL | 1.4227 mL | 2.8455 mL | 7.1137 mL | |
| 20 mM | 0.2134 mL | 1.0671 mL | 2.1341 mL | 5.3353 mL | |
| 25 mM | 0.1707 mL | 0.8536 mL | 1.7073 mL | 4.2682 mL | |
| 30 mM | 0.1423 mL | 0.7114 mL | 1.4227 mL | 3.5568 mL | |
| 40 mM | 0.1067 mL | 0.5335 mL | 1.0671 mL | 2.6676 mL | |
| 50 mM | 0.0854 mL | 0.4268 mL | 0.8536 mL | 2.1341 mL | |
| 60 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7784 mL | |
| 80 mM | 0.0534 mL | 0.2668 mL | 0.5335 mL | 1.3338 mL | |
| 100 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0671 mL |
Stiripentol Related Classifications
HY-103392 Related Classifications
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