EMD 386088 free base
EMD386088 free base is a potent serotonin 6 receptor (5-HT6R) agonist. EMD386088 free base induces cell death. EMD386088 free base regulates the activity of ERK1/2. EMD386088 free base has the potential for the research of alzheimer's disease (AD) and schizophrenia.
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- CAS No.: 54635-62-0
- Formule: C14H15ClN2
- Masse moléculaire:246.74
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
5-HT6 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
7.4 nM
Compound: 18
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Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
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[PMID: 16055331] |
In Vitro
EMD386088 free base (1, 10, 60 μM; 0-18 h) induces cell death in a dose- and time- dependent manner[1].
EMD386088 free base (1, 10, 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:
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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 free base (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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CAS No. 54635-62-0
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Masse moléculaire 246.74
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Formule C14H15ClN2
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SMILES
CC(N1)=C(C2=CCNCC2)C3=C1C=CC(Cl)=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EMD 386088 free base Related Classifications
HY-103130A Related Classifications
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