Carbamazepine (CBZ), topiramate (TPR), stiripentol (STP), pentylenetetrazole (PTZ), 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and DL-2-amino-5-phosphonopentanoic acid (APV) were purchased from Sigma-Aldrich, sodium valproate (VPA) from Sanofi-Aventis, clobazam (CLB) from Lipomed AG, Switzerland and fenfluramine (FA) from Peak International Products B.V. Compounds were dissolved in DMSO and diluted in embryo medium to achieve a final DMSO concentration of 1% w/v, which served as a vehicle control (VHC). In case of treatment for the hyperthermia-experiment, a final DMSO concentration of 0.1% w/v was used.
Stiripentol
Manufactured by Merck Group
Sourced in United States
Stiripentol is a chemical compound used as a pharmaceutical ingredient in various medical products. It is a white crystalline powder that functions as an anticonvulsant medication. Stiripentol is primarily utilized in the treatment of certain types of epilepsy.
Automatically generated - may contain errors
Lab products found in correlation
Carbamazepine, by Merck Group (4 mentions)
Topiramate, by Merck Group (3 mentions)
Clobazam, by Merck Group (3 mentions)
Phenobarbital, by Merck Group (2 mentions)
Lamotrigine, by Merck Group (2 mentions)
Levetiracetam, by Merck Group (2 mentions)
Pentylenetetrazole, by Merck Group (1 mentions)
Dl 2 amino 5 phosphonopentanoic acid, by Merck Group (1 mentions)
6 cyano 7 nitroquinoxaline 2 3 dione, by Merck Group (1 mentions)
Bumetanide, by Merck Group (1 mentions)
Midazolam, by Merck Group (1 mentions)
Clonazepam, by Merck Group (1 mentions)
Ethosuximide, by Merck Group (1 mentions)
Sodium valproate, by Merck Group (1 mentions)
Lamotrigine, by AK Scientific (1 mentions)
Phenytoin, by Merck Group (1 mentions)
Eslicarbazepine, by Tokyo Chemical Industry (1 mentions)
Gabapentin, by Tokyo Chemical Industry (1 mentions)
Levetiracetam, by Tokyo Chemical Industry (1 mentions)
Rufinamide, by Tokyo Chemical Industry (1 mentions)
9 protocols using stiripentol
1
Anticonvulsant Compounds: Preparation and Use
2
Glutamate/Glycine-Induced Calcium Signaling
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Coverslips were mounted on a closed perfusion chamber used to apply different media to the cells. Standard media (ACSF) consisted of HEPES-buffered standard physiological perfusion medium14 (link) and containing NaCl 140 mM, KCl 3 mM, CaCl2 3 mM, MgCl2 2 mM, Glucose 5 mM, HEPES 10 mM, adjusted to a pH of 7.3 with NaOH.
All experiments were performed at room temperature. Glutamate, Glycine, D-Serine, L-Lactate, D-Lactate, Pyruvate, MK801, Ifenprodil, dithiothreitol (DTT), 5,5′-dithiobis(2-nitrobenzoic acid) (DTNB), Stiripentol were provided by Sigma-Aldrich and added to ACSF. For most experiments, 2 successive pulses of glutamate (1–100 μM) and glycine (100 μM) are applied to the cells spaced out by a minimum delay of 20 min. The amplitude of the 1st and the 2nd Ca2+ response induced by the glutamate/glycine cocktail are compared. For the experiments performed at 1 mM of glutamate (+100 μM of glycine), only a single pulse is applied due to a higher number of excito-toxic responses. Finally, for some experiments, 5 mM of Glucose are added to the ACSF (final concentration of Glucose: 10 mM; annotated 5 mM extra Glucose ACSF).
All experiments were performed at room temperature. Glutamate, Glycine, D-Serine, L-Lactate, D-Lactate, Pyruvate, MK801, Ifenprodil, dithiothreitol (DTT), 5,5′-dithiobis(2-nitrobenzoic acid) (DTNB), Stiripentol were provided by Sigma-Aldrich and added to ACSF. For most experiments, 2 successive pulses of glutamate (1–100 μM) and glycine (100 μM) are applied to the cells spaced out by a minimum delay of 20 min. The amplitude of the 1st and the 2nd Ca2+ response induced by the glutamate/glycine cocktail are compared. For the experiments performed at 1 mM of glutamate (+100 μM of glycine), only a single pulse is applied due to a higher number of excito-toxic responses. Finally, for some experiments, 5 mM of Glucose are added to the ACSF (final concentration of Glucose: 10 mM; annotated 5 mM extra Glucose ACSF).
3
Antiepileptic Drug Stock Solution Protocol
4
Fenofibric Acid Formulation Development
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FN was obtained from Enhua Pharma Co., Ltd (Xuzhou, People’s Republic of China), and fenofibric acid was purchased from Xingyuan Chemicals (Zhengzhou, People’s Republic of China). Stiripentol (4,4-dimethyl-1- [3,4(methylenedioxy)-phenyl]-1-penten-3-ol) was from Sigma-Aldrich (St Louis, MO, USA). Lauroyl polyoxyl-6 glycerides (LPG) (Labrafil M2130 CS) and glyceryl distearate (Precirol ATO 5) were kindly provided by Gattefossé Co. (Saint Priest, Cedex, France). Lipase from porcine pancreas (>20,000 units/mg) and PEG monooleate (Mn ~860) were bought from Aladdin Reagent (Shanghai, People’s Republic of China). Tween 80 was supplied by Aladdin Reagent. High-performance liquid chromatography (HPLC)-grade methanol was provided by Merck (Darmstadt, Germany). Deionized water was prepared by a water purifier (Chengdu, People’s Republic of China). All other chemicals were of analytical grade and used as received.
5
Anticonvulsant Compound Preparation and Dosing
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Valproate (VPA), topiramate (TPM), stiripentol (STP), cannabidiol (CBD), clobazam (CLB), levetiracetam (LEV), carbamazepine (CBZ), and lamotrigine (LTG) were purchased from Sigma-Aldrich. Phenytoin (PHT) was from Acros Organics. (±)-Fenfluramine [(±)-FFA] was a gift from Prof. Berten Ceulemans (University of Antwerp, Belgium). The enantiomers of FFA and norfenfluramine (norFFA) were provided by Zogenix International (Emeryville, USA). Compounds were dissolved in dimethylsulfoxide (DMSO), and diluted in embryo medium to achieve a final DMSO concentration of 0.1% w/v. Embryo medium with 0.1% w/v DMSO served as a vehicle control (VHC).
6
Acute Administration of Antiepileptic Drugs
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Carbamazepine, clobazam, lamotrigine, levetiracetam, phenobarbital, topiramate, and valproic acid were purchased from Sigma‐Aldrich Co. (St. Louis, MO). Stiripentol (Sigma‐Aldrich Co.; Cayman Chemical, Ann Arbor, MI) and phenytoin sodium solution (X‐Gen Pharmaceuticals, Horseheads, NV) were also used. For acute administration, drugs were prepared as solutions with the following vehicles: A‐ saline (levetiracetam, phenobarbital, topiramate, valproic acid); B‐ 0.5% methylcellulose in water (phenytoin); C‐ 5% hydroxypropyl‐β‐cyclodextrin (Carbamazepine, lamotrigine); and D‐ vegetable oil (clobazam, Stiripentol). All drugs were administered as a single intraperitoneal (ip) injection in a volume of 10 mL/kg. The following acute doses resulted in plasma concentrations within the human therapeutic range (Table 1 ): 20 mg/kg Carbamazepine, 5 mg/kg clobazam, 20 mg/kg lamotrigine, 10 mg/kg levetiracetam, 15 mg/kg phenobarbital, 15 mg/kg phenytoin, 40 mg/kg topiramate, 25 mg/kg Stiripentol, 75 mg/kg valproic acid, and 0.1–10 mg/kg clobazam plus 25 mg/kg Stiripentol. Acute toxicity was not observed with any drugs at the administered doses.
7
Comprehensive LDH Inhibitor Library
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All LDH inhibitors (AT-101 (Catalog #SML0433, ≥98%), FX-11 (Catalog #427218, ≥96%), galloflavin (Catalog #SML0776, ≥95%), gossypol (Catalog #G8761, ≥95%), GSK2837808A (Catalog #5.33660, ≥95%), isosafrole (Catalog #329606, ≥100%), sodium oxamate (Catalog #02751, ≥98%), stiripentol (Catalog #S6826, ≥98%), and NHI-2 (Catalog #SML1463, ≥98%)) were purchased from Sigma-Aldrich (Burlington, MA, USA).
8
Multicompound Anti-Cancer Screening
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Doxycycline, Ascorbic Acid, 2-Deoxy-D-glucose (2-DG), Irinotecan, Berberine Chloride, Niclosamide, Chloroquine diphosphate, Stiripentol and Atovaquone were all purchased from Sigma Aldrich. Sorafenib was obtained from Generon. All compounds were dissolved in DMSO, except Ascorbic Acid, 2-deoxy-D-glucose (2-DG) and Chloroquine diphosphate, which were dissolved in cell culture medium.
9
Establishing TMZ-resistant GBM Cell Lines
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The patient‐derived xenograft GBM primary cell line TBD0220 derived from a female GBM patient with no history of radiation therapy or chemotherapy and underwent surgery at Hebei University‐affiliated hospital,[32 (link)
] and GBM cell line U87 was procured from the cell bank of the Chinese Academy of Sciences. TMZ‐resistant cells (TBD0220TR and U87TR) were derived from TBD0220 and U87 cells. All cells were maintained at 37 °C with 100% humidity and 5% CO2. Briefly, TBD0220 and U87 cells were exposed to a concentration of TMZ that was gradually increased from 1.25 mmol L−1 to a maximal dose of 160 mmol L−1. During the first induction phase, the culture media containing TMZ was replaced every 72 h. The concentration of TMZ was increased after maintaining the initial dose for 14 days and observing consistent cell growth. At each incremental step, the cultures were maintained for three to four weeks. The overall procedure took half a year.[33 (link)
] To maintain authenticity, all GBM cell lines were cryopreserved in liquid nitrogen. TBD0220 and TBD0220TR cells were cultivated in DMEM/F12 (Gibco) with 10% FBS, whereas U87 and U87TR cells were cultured in DMEM (Gibco) with 10% FBS. TMZ (#HY‐17364) and stiripentol (#HY‐103392) were acquired from MedChemExpress (China). TMZ and stiripentol were dissolved in DMSO (Sigma‐Aldrich, D2650, USA) to treat GBM cells.
] and GBM cell line U87 was procured from the cell bank of the Chinese Academy of Sciences. TMZ‐resistant cells (TBD0220TR and U87TR) were derived from TBD0220 and U87 cells. All cells were maintained at 37 °C with 100% humidity and 5% CO2. Briefly, TBD0220 and U87 cells were exposed to a concentration of TMZ that was gradually increased from 1.25 mmol L−1 to a maximal dose of 160 mmol L−1. During the first induction phase, the culture media containing TMZ was replaced every 72 h. The concentration of TMZ was increased after maintaining the initial dose for 14 days and observing consistent cell growth. At each incremental step, the cultures were maintained for three to four weeks. The overall procedure took half a year.[33 (link)
] To maintain authenticity, all GBM cell lines were cryopreserved in liquid nitrogen. TBD0220 and TBD0220TR cells were cultivated in DMEM/F12 (Gibco) with 10% FBS, whereas U87 and U87TR cells were cultured in DMEM (Gibco) with 10% FBS. TMZ (#HY‐17364) and stiripentol (#HY‐103392) were acquired from MedChemExpress (China). TMZ and stiripentol were dissolved in DMSO (Sigma‐Aldrich, D2650, USA) to treat GBM cells.
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