Carabersat
Based on 1 Customer Validation
Carabersat is a potent anticonvulsant agent.
For research use only. We do not sell to patients.
- Purity: 98.22%
- CAS No.: 184653-84-7
- Formula: C20H20FNO4
- Molecular Weight:357.38
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
[3H]Carabersat ([3H]SB 204269) binds to rat forebrain membranes with moderate affinity (Kd 40 nM) and pKi values of 7.3[1]. Carabersat is able to bind to mouse forebrain membranes, and the binding is saturable and stereospecific, with a Kd of 53 nM. The labelled [3H]Carabersat produces a Kd of 32 nM[2]. Carabersat (SB-204269, 1-100 μM) has no effect on Na+ current in cultured hippocampal neurones. Carabersat also shows no effect on action potential discharges evoked by elevating external K+[3]. Carabersat (SB-204269) is structurally-related to the benzopyran ATP-sensitive potassium channel (KATP) opener, cromakalim, but has opposite stereochemistry, and the mechanism of action of Carabersat is not thought to involve KATP[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 184653-84-7
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Appearance Solid
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Molecular Weight 357.38
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Formula C20H20FNO4
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Color White to off-white
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SMILES
O=C(N[C@@H]1[C@@H](O)C(C)(C)OC2=CC=C(C(C)=O)C=C12)C3=CC=C(F)C=C3
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Synonyms
SB-204269
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 200 mg/mL (559.63 mM; Need ultrasonic; 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, 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.
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.
Protocol
Mice[1]
In this model, groups of 10-20 naive mice (25-30 g) are assessed for production of a tonic hindlimb extension seizure following a single corneal electroshock using an "up and down" method of shock titration. The effects of drug treatment are expressed as a percentage change from vehicle control values and statistical comparisons between groups are made. Carabersat is administered orally as a fine suspension in 1% methylcellulose one hour before electroshock application[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[2]. Herdon H, et al. The novel anticonvulsant SB 204269 binds to a stereospecific site in the mouse brain. Eur J Pharmacol. 1996 Oct 31;314(3):R7-8. [Content Brief]
[3]. Caeser M, et al. Lack of effect of the novel anticonvulsant SB-204269 on voltage-dependent currents in neurones cultured from rat hippocampus. Neurosci Lett. 1999 Aug 13;271(1):57-60. [Content Brief]
[4]. Crespi F, et al. SB-204269 SmithKline Beecham. IDrugs. 1998 Sep;1(5):595-8. [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 | 2.7981 mL | 13.9907 mL | 27.9814 mL | 69.9535 mL |
| 5 mM | 0.5596 mL | 2.7981 mL | 5.5963 mL | 13.9907 mL | |
| 10 mM | 0.2798 mL | 1.3991 mL | 2.7981 mL | 6.9954 mL | |
| 15 mM | 0.1865 mL | 0.9327 mL | 1.8654 mL | 4.6636 mL | |
| 20 mM | 0.1399 mL | 0.6995 mL | 1.3991 mL | 3.4977 mL | |
| 25 mM | 0.1119 mL | 0.5596 mL | 1.1193 mL | 2.7981 mL | |
| 30 mM | 0.0933 mL | 0.4664 mL | 0.9327 mL | 2.3318 mL | |
| 40 mM | 0.0700 mL | 0.3498 mL | 0.6995 mL | 1.7488 mL | |
| 50 mM | 0.0560 mL | 0.2798 mL | 0.5596 mL | 1.3991 mL | |
| 60 mM | 0.0466 mL | 0.2332 mL | 0.4664 mL | 1.1659 mL | |
| 80 mM | 0.0350 mL | 0.1749 mL | 0.3498 mL | 0.8744 mL | |
| 100 mM | 0.0280 mL | 0.1399 mL | 0.2798 mL | 0.6995 mL |
Carabersat Related Classifications
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