SB357134
Based on 1 Customer Validation
SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats.
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- Pureté : 99.4%
- CAS No.: 219963-52-7
- Formule: C17H18Br2FN3O3S
- Masse moléculaire:523.21
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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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Help & FAQs
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Activité biologique
Description
IC50 & Target
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5-HT6 Receptor |
In Vitro
SB-357134 (0.1, 0.3, 1, and 3 μM) concentration-dependently inhibits the 5-HT-mediated increased level of cAMP, which is surmountable at high 5-HT concentrations, consistent with competitive antagonism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
SB-357134 (0.03-30 mg/kg; 0-24 h; p.o.; single dose) produces a potent and dose-related anticonvulsant effect in the rat MEST model, with a minimum significantly effective dose of 0.1 mg/kg[1].
Chronic administration of SB-357134 (10 mg/kg; p.o.; twice daily; 7 days) significantly shortens path length compared to vehicle and acute administration of SB-357134[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague–Dawley rats[1]
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Dosage:0.03–30 mg/kg
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Administration:0-24 h; p.o.; 0.03–30 mg/kg
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Result:Produced a potent and dose-related anticonvulsant effect in the rat MEST model, with a minimum significantly effective dose of 0.1 mg/kg. Increased seizure threshold up to 123±12% at the highest dose tested of 30 mg/kg. At 10 mg/kg, exhibited a rapid onset of action, significantly increasing seizure threshold from a control value of 21.7 to 26.7 mA at 1 h postdose. Observed Peak activity within 4–6 h postdose. With the exception of an unexplained loss of activity at 12 h, had a long duration of action of 21 h in this model.
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Animal Model:Sprague–Dawley rats[1]
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Dosage:10 mg/kg
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Administration:10 mg/kg; p.o.; twice daily; 7 days
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Result:Significantly shortened path length when administered chronically compared to vehicle and administered acutely.
Chemical Information
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CAS No. 219963-52-7
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Appearance Solid
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Masse moléculaire 523.21
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Formule C17H18Br2FN3O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(C(N2CCNCC2)=C1)OC)(NC3=CC(Br)=CC(F)=C3Br)=O
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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
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (191.13 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, 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)
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: ≥ 5 mg/mL (9.56 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 1.9113 mL | 9.5564 mL | 19.1128 mL | 47.7820 mL |
| 5 mM | 0.3823 mL | 1.9113 mL | 3.8226 mL | 9.5564 mL | |
| 10 mM | 0.1911 mL | 0.9556 mL | 1.9113 mL | 4.7782 mL | |
| 15 mM | 0.1274 mL | 0.6371 mL | 1.2742 mL | 3.1855 mL | |
| 20 mM | 0.0956 mL | 0.4778 mL | 0.9556 mL | 2.3891 mL | |
| 25 mM | 0.0765 mL | 0.3823 mL | 0.7645 mL | 1.9113 mL | |
| 30 mM | 0.0637 mL | 0.3185 mL | 0.6371 mL | 1.5927 mL | |
| 40 mM | 0.0478 mL | 0.2389 mL | 0.4778 mL | 1.1945 mL | |
| 50 mM | 0.0382 mL | 0.1911 mL | 0.3823 mL | 0.9556 mL | |
| 60 mM | 0.0319 mL | 0.1593 mL | 0.3185 mL | 0.7964 mL | |
| 80 mM | 0.0239 mL | 0.1195 mL | 0.2389 mL | 0.5973 mL | |
| 100 mM | 0.0191 mL | 0.0956 mL | 0.1911 mL | 0.4778 mL |
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