EMD 386088 free base

Cat. No.: HY-103130A: Data Sheet Handling Instructions
FAQs
Technical Support

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.

For research use only. We do not sell to patients.

EMD 386088 free base Chemical Structure

CAS No. : 54635-62-0

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of EMD 386088 free base:

EMD386088

Other Forms of EMD 386088 free base:

EMD386088 In-stock

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

5-HT₆ Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	7.4 nM Compound: 18	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	[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.

Cell Viability Assay^[1]

Cell Line:	HEK/HA-5-HT6R, native HEK293 cells
Concentration:	1, 10, 60 μM
Incubation Time:	0-18 h
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.

Western Blot Analysis^[1]

Cell Line:	HEK/HA-5-HT6R, native HEK293 cells
Concentration:	1, 10, 60 μM
Incubation Time:
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 (1, 5, 10 mg/kg) impairs both short-term memory (STM) and long-term memory (LTM) at 5 mg/kg, but produces no significant effects at 10 mg/kg in male Wistar rats^[2].
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.

Molecular Weight

246.74

Formula

C₁₄H₁₅ClN₂

CAS No.

54635-62-0

SMILES

CC(N1)=C(C2=CCNCC2)C3=C1C=CC(Cl)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]