Carisbamate
Based on 1 publication(s) in Google Scholar
Carisbamate (RWJ-333369) is an orally active neuromodulator. Carisbamate prevents the development and production of epilep-like discharges and has a neuroprotective effect after in vitro epilepticus-like injury. Carisbamate has good antiepileptic activity in genetic models of generalized and nonconvulsive epilepsy.
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- Pureté: 98.75%
- CAS No.: 194085-75-1
- Formule: C9H10ClNO3
- Masse moléculaire:215.64
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Carisbamate
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Activité biologique
Carisbamate (200 μM; 12 h) exhibits antiepileptic effects on SREDs model of hippocampal cells[1].
Carisbamate (200 μM; 24 h) shows long lasting effects on the hippocampal neurons that are independent from antiepileptic effects in vitro[1].
Carisbamate not only inhibits the development and expression of SREDs in the majority of neurons, but also decreases seizure frequency and duration in the few neurons that still has an occasional epileptiform event[1].
Carisbamate (200 μM) shows neuroprotective effects on hippocampal cells with SE (status epilepticus)-like injury[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hippocampal cells (from 2-day postnatal Sprague-Dawley rat; spontaneous recurrent epileptiform discharges (SREDs) model)
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Concentration:200 µM
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Incubation Time:12 h
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Result:Acutely inhibited SREDs with greater than 95% of the neurons exhibited an in vitro antiepileptic effect.
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Cell Line:Hippocampal cells (SREDs model)
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Concentration:200 µM
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Incubation Time:24 h
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Result:Exhibited cells evaluated the day after treatment were still free of in vitro seizure activity and did not develop SREDs.
Carisbamate (20, 30 mg/kg; i.p.; single) shows no wild running episode or tonic seizure occurres in any of the rats tested[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male genetic absence epilepsy rat (absence seizures model)[2].
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Dosage:10, 30, 60 mg/kg
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Administration:Intraperitoneal injection; single.
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Result:Completely inhibited SWD when at 60 mg/kg after 120 min, and restored the duration of SWD to the control level when at 30 mg/kg after 100 min.
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Animal Model:Male Wistar audiogenic sensitive rat (convulsive seizures model)[2].
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Dosage:10, 20, 30 mg/kg
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Administration:Intraperitoneal injection; single.
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Result:Showed no wild running episode or tonic seizure occurred in any of the rats tested when at 20 and 30 mg/kg.
Increased by 327% the latency to the tonic seizure that still occurred in the six of eight rats studied when at 10 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 194085-75-1
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Appearance Solid
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Masse moléculaire 215.64
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Formule C9H10ClNO3
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Color White to off-white
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SMILES
NC(OC[C@H](C1=CC=CC=C1Cl)O)=O
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Synonyms
RWJ-333369
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576
Solvant et solubilité
DMSO : ≥ 100 mg/mL (463.74 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (11.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (11.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Deshpande LS, et al. Carisbamate prevents the development and expression of spontaneous recurrent epileptiform discharges and is neuroprotective in cultured hippocampal neurons. Epilepsia. 2008 Oct;49(10):1795-802. [Content Brief]
[2]. François J, et al. Effects of carisbamate (RWJ-333369) in two models of genetically determined generalized epilepsy, the GAERS and the audiogenic Wistar AS. Epilepsia. 2008 Mar;49(3):393-9. [Content Brief]
[3]. Novak GP, et al. Carisbamate (RWJ-333369). Neurotherapeutics. 2007 Jan;4(1):106-9. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.6374 mL | 23.1872 mL | 46.3744 mL | 115.9361 mL |
| 5 mM | 0.9275 mL | 4.6374 mL | 9.2749 mL | 23.1872 mL | |
| 10 mM | 0.4637 mL | 2.3187 mL | 4.6374 mL | 11.5936 mL | |
| 15 mM | 0.3092 mL | 1.5458 mL | 3.0916 mL | 7.7291 mL | |
| 20 mM | 0.2319 mL | 1.1594 mL | 2.3187 mL | 5.7968 mL | |
| 25 mM | 0.1855 mL | 0.9275 mL | 1.8550 mL | 4.6374 mL | |
| 30 mM | 0.1546 mL | 0.7729 mL | 1.5458 mL | 3.8645 mL | |
| 40 mM | 0.1159 mL | 0.5797 mL | 1.1594 mL | 2.8984 mL | |
| 50 mM | 0.0927 mL | 0.4637 mL | 0.9275 mL | 2.3187 mL | |
| 60 mM | 0.0773 mL | 0.3865 mL | 0.7729 mL | 1.9323 mL | |
| 80 mM | 0.0580 mL | 0.2898 mL | 0.5797 mL | 1.4492 mL | |
| 100 mM | 0.0464 mL | 0.2319 mL | 0.4637 mL | 1.1594 mL |
Carisbamate Related Classifications
HY-14948 Related Classifications
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