2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. EMD386088

EMD386088 is a potent serotonin 6 receptor (5-HT6R) agonist. EMD386088 induces cell death. EMD386088 regulates the activity of ERK1/2. EMD386088 has the potential for the research of alzheimer's disease (AD) and schizophrenia.

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EMD386088 Chemical Structure

EMD386088 Chemical Structure

CAS No. : 1171123-46-8

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5 mg USD 312 In-stock
10 mg USD 499 In-stock
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Based on 1 publication(s) in Google Scholar

EMD386088 Related Antibodies

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Description

EMD386088 is a potent serotonin 6 receptor (5-HT6R) agonist. EMD386088 induces cell death. EMD386088 regulates the activity of ERK1/2. EMD386088 has the potential for the research of alzheimer's disease (AD) and schizophrenia[1][2][3].

IC50 & Target[1]

5-HT6 Receptor

 

In Vitro

EMD386088 (1, 10, 60 μM; 0-18 h) induces cell death in a dose- and time- dependent manner[1].
EMD386088 (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.

EMD386088 Related Antibodies

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: 0-18 h
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 (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 (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

283.20

Formula

C14H16Cl2N2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(N1)=C(C2=CCNCC2)C3=C1C=CC(Cl)=C3.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5311 mL 17.6554 mL 35.3107 mL
5 mM 0.7062 mL 3.5311 mL 7.0621 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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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EMD386088 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EMD3860881171123-46-8EMD 386088EMD-3860885-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorcell deathERK1/2alzheimer's diseaseschizophreniaHEK/HA-5-HT6Rnative HEK293 cellsInhibitorinhibitorinhibit

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