S 18986
Based on 1 Customer Validation
S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
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- Pureza: 99.90%
- No. CAS: 175340-20-2
- Fòrmula: C10H12N2O2S
- Peso molecular:224.28
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Almacenamiento:Powder -20°C, 3 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Ver todos los productos específicos de isoformas iGluR
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Oocyte | EC50 |
130 μM
Compound: 4
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Activity at Wistar rat cortex AMPA receptor expressed in Xenopus laevis oocytes assessed as effect on (S)-AMPA-induced current
Activity at Wistar rat cortex AMPA receptor expressed in Xenopus laevis oocytes assessed as effect on (S)-AMPA-induced current
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[PMID: 17552506] |
S 18986 (5-50 mg/kg; i.p.) significantly increases both the induction and the maintenance of 4 and 20 bursts tetanus-evoked potentiation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Middle-aged (14-15-months-old) mice[1]
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Dosage:0.3, 1, and 10 mg/kg
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Administration:p.o.
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Result:Showed antiamnesic properties in middle-aged rodents.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 175340-20-2
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Appearance Solid
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Peso molecular 224.28
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Fòrmula C10H12N2O2S
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Color White to light yellow
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SMILES
O=S1(C2=CC=CC=C2N3[C@@](CCC3)([H])N1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (445.87 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 (11.15 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 (11.15 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.
Pureza y Documentación
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Ficha de datos (281 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bernard K, et al. DRUG FOCUS: S 18986: A positive allosteric modulator of AMPA-type glutamate receptorspharmacological profile of a novel cognitive enhancer. CNS Neurosci Ther. 2010 Oct;16(5):e193-212. [Content Brief]
[2]. Bourasset F, et al. Neuropharmacokinetics of a new alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) modulator, S18986 [(S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide], in the rat. Drug Metab Dispos. 2005 Aug;33(8):1137-43. [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 | 4.4587 mL | 22.2936 mL | 44.5871 mL | 111.4678 mL |
| 5 mM | 0.8917 mL | 4.4587 mL | 8.9174 mL | 22.2936 mL | |
| 10 mM | 0.4459 mL | 2.2294 mL | 4.4587 mL | 11.1468 mL | |
| 15 mM | 0.2972 mL | 1.4862 mL | 2.9725 mL | 7.4312 mL | |
| 20 mM | 0.2229 mL | 1.1147 mL | 2.2294 mL | 5.5734 mL | |
| 25 mM | 0.1783 mL | 0.8917 mL | 1.7835 mL | 4.4587 mL | |
| 30 mM | 0.1486 mL | 0.7431 mL | 1.4862 mL | 3.7156 mL | |
| 40 mM | 0.1115 mL | 0.5573 mL | 1.1147 mL | 2.7867 mL | |
| 50 mM | 0.0892 mL | 0.4459 mL | 0.8917 mL | 2.2294 mL | |
| 60 mM | 0.0743 mL | 0.3716 mL | 0.7431 mL | 1.8578 mL | |
| 80 mM | 0.0557 mL | 0.2787 mL | 0.5573 mL | 1.3933 mL | |
| 100 mM | 0.0446 mL | 0.2229 mL | 0.4459 mL | 1.1147 mL |
S 18986 Related Classifications
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