2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. WAY-181187

WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.

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WAY-181187 Chemical Structure

WAY-181187 Chemical Structure

CAS No. : 554403-49-5

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1 mg USD 157 In-stock
5 mg USD 330 In-stock
10 mg USD 550 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM[1]. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist[2].

IC50 & Target[1]

5-HT6 Receptor

2.2 nM (Ki)

5-HT6 Receptor

6.6 nM (EC50)

In Vitro

WAY181187 (1 and 10 μM) increases activation of ERK1/2. WAY181187 also increases Fyn kinase activity[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

WAY-181187 Related Antibodies

Western Blot Analysis[2]

Cell Line: HEK/HA-5-HT6 receptor cells
Concentration: 1 and 10 μM
Incubation Time: Pretreatment 5 minutes
Result: Increased activation of ERK1/2 both at 1 and 10 μM concentrations.
In Vivo

Acute administration of WAY-181187 (3-30 mg/kg, s.c.) significantly increases extracellular GABA concentrations without altering the levels of glutamate or norepinephrine in the rat frontal cortex. Additionally, WAY-181187 (30 mg/kg, s.c.) produces modest yet significant decreases in cortical dopamine and 5-HT levels[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male Sprague-Dawley rats weighing 280–350 g[1]
Dosage: 3, 10, or 30 mg/kg
Administration: Acute dministered by s.c.
Result: Significantly increased extracellular GABA concentrations without altering the levels of glutamate or norepinephrine.
Molecular Weight

380.87

Formula

C15H13ClN4O2S2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

NCCC1=CN(S(=O)(C2=C(Cl)N=C3SC=CN32)=O)C4=C1C=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (262.56 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 2.6256 mL 13.1278 mL 26.2557 mL
5 mM 0.5251 mL 2.6256 mL 5.2511 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. 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
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Volume
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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 (6.56 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.56 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
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).
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. 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 2.6256 mL 13.1278 mL 26.2557 mL 65.6392 mL
5 mM 0.5251 mL 2.6256 mL 5.2511 mL 13.1278 mL
10 mM 0.2626 mL 1.3128 mL 2.6256 mL 6.5639 mL
15 mM 0.1750 mL 0.8752 mL 1.7504 mL 4.3759 mL
20 mM 0.1313 mL 0.6564 mL 1.3128 mL 3.2820 mL
25 mM 0.1050 mL 0.5251 mL 1.0502 mL 2.6256 mL
30 mM 0.0875 mL 0.4376 mL 0.8752 mL 2.1880 mL
40 mM 0.0656 mL 0.3282 mL 0.6564 mL 1.6410 mL
50 mM 0.0525 mL 0.2626 mL 0.5251 mL 1.3128 mL
60 mM 0.0438 mL 0.2188 mL 0.4376 mL 1.0940 mL
80 mM 0.0328 mL 0.1641 mL 0.3282 mL 0.8205 mL
100 mM 0.0263 mL 0.1313 mL 0.2626 mL 0.6564 mL
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WAY-181187 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:

WAY-181187554403-49-5SAX-187WAY181187WAY 181187SAX187SAX 1875-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptoranxietyrelateddisordersOCD5-HT6cAMPFynERK1/2Inhibitorinhibitorinhibit

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