EMD386088
Based on 1 Customer Validation
EMD386088 is a potent and selective 5-HT6 receptor (5-HT6R) agonist with an EC50 of 1.0 nM. EMD-386088 is inactive against other HT receptors except 5-HT3R (IC50 of 34 nM). EMD386088 regulates the activity of ERK1/2. EMD386088 has the potential for the research of alzheimer's disease (AD) and schizophrenia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.06%
- No. CAS: 1171123-46-8
- Fòrmula: C14H16Cl2N2
- Peso molecular:283.20
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
5-HT6 Receptor |
In Vitro
EMD386088 (1-60 μM; 0-18 h) induces cell death with cytotoxicity in a dose- and time- dependent manner[1].
EMD386088 (1-60 μM) regulates the activity of ERK1/2 in a 5-HT6R-dependent and 5-HT6R-independent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK/HA-5-HT6R, native HEK293 cells
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Concentration:1, 10, 60 μM
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Incubation Time:0-18 h
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Result:Induced cell death in HEK293 cells stably expressing HA-5-HT6R (HEK/HA-5-HT6R) and in native HEK293 cells in a dose- and time- dependent manner.
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Cell Line:HEK/HA-5-HT6R, native HEK293 cells
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Concentration:1, 10, 60 μM
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Incubation Time:0-18 h
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Result:Led to the activation of ERK1/2 at 0-30 μM, retarded ERK1/2 activation at a high dose of 60 μM in HEK/HA-5-HT6R cells.
In Vivo
EMD386088 (0, 2, 4 mg/kg) significantly impairs spontaneous alternation performancein at 2 mg/kg, but the high dose of 4 mg/kg dose not reach significance in C57BL/6J mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1171123-46-8
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Appearance Solid
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Peso molecular 283.20
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Fòrmula C14H16Cl2N2
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Color Light yellow to yellow
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SMILES
CC(N1)=C(C2=CCNCC2)C3=C1C=CC(Cl)=C3.[H]Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (353.11 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.5 mg/mL (8.83 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (280 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Yun HM, et al. 5-HT6 receptor ligands, EMD386088 and SB258585, differentially regulate 5-HT6 receptor-independent events. Toxicol In Vitro. 2011 Dec;25(8):2035-40. [Content Brief]
[2]. Meneses A, et al. The effects of the 5-HT(6) receptor agonist EMD and the 5-HT(7) receptor agonist AS19 on memory formation. Behav Brain Res. 2008 Dec 16;195(1):112-9. [Content Brief]
[3]. Amodeo DA, et al. 5-HT6 receptor agonist EMD386088 impairs behavioral flexibility and working memory. Behav Brain Res. 2018 Sep 3;349:8-15. [Content Brief]
[4]. Mattsson C, et al. 2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4230-4. [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 (sealed storage, away from moisture). 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 | 3.5311 mL | 17.6554 mL | 35.3107 mL | 88.2768 mL |
| 5 mM | 0.7062 mL | 3.5311 mL | 7.0621 mL | 17.6554 mL | |
| 10 mM | 0.3531 mL | 1.7655 mL | 3.5311 mL | 8.8277 mL | |
| 15 mM | 0.2354 mL | 1.1770 mL | 2.3540 mL | 5.8851 mL | |
| 20 mM | 0.1766 mL | 0.8828 mL | 1.7655 mL | 4.4138 mL | |
| 25 mM | 0.1412 mL | 0.7062 mL | 1.4124 mL | 3.5311 mL | |
| 30 mM | 0.1177 mL | 0.5885 mL | 1.1770 mL | 2.9426 mL | |
| 40 mM | 0.0883 mL | 0.4414 mL | 0.8828 mL | 2.2069 mL | |
| 50 mM | 0.0706 mL | 0.3531 mL | 0.7062 mL | 1.7655 mL | |
| 60 mM | 0.0589 mL | 0.2943 mL | 0.5885 mL | 1.4713 mL | |
| 80 mM | 0.0441 mL | 0.2207 mL | 0.4414 mL | 1.1035 mL | |
| 100 mM | 0.0353 mL | 0.1766 mL | 0.3531 mL | 0.8828 mL |
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