WAY-181187
Based on 2 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 98.83%
- CAS No.: 554403-49-5
- Formula: C15H13ClN4O2S2
- Molecular Weight:380.87
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) WAY-181187
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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5-HT6 Receptor |
5-HT6 Receptor 2.2 nM (Ki) |
5-HT6 Receptor 6.6 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| HeLa | EC50 |
6.5 nM
Compound: 16
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Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as induction of cAMP production after 10 mins by radioimmunoassay
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[PMID: 19739674] |
| HeLa | EC50 |
6.5 nM
Compound: 11q
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Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
Agonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
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[PMID: 17948978] |
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.
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Cell Line:HEK/HA-5-HT6 receptor cells
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Concentration:1 and 10 μM
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Incubation Time:Pretreatment 5 minutes
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Result:Increased activation of ERK1/2 both at 1 and 10 μM concentrations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague-Dawley rats weighing 280–350 g[1]
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Dosage:3, 10, or 30 mg/kg
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Administration:Acute dministered by s.c.
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Result:Significantly increased extracellular GABA concentrations without altering the levels of glutamate or norepinephrine.
Chemical Information
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CAS No. 554403-49-5
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Appearance Solid
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Molecular Weight 380.87
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Formula C15H13ClN4O2S2
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Color White to yellow
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SMILES
NCCC1=CN(S(=O)(C2=C(Cl)N=C3SC=CN32)=O)C4=C1C=CC=C4
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Synonyms
SAX-187
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Thromb Res
2024 May:237:1-13. PMID: 38513536 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (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.
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.
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.
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.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Lee E Schechter, et al. Neuropharmacological Profile of Novel and Selective 5-HT6 Receptor Agonists: WAY-181187 and WAY-208466. Neuropsychopharmacology. 2008 May;33(6):1323-35. [Content Brief]
[2]. Teresa Riccioni, et al. ST1936 Stimulates cAMP, Ca2+, ERK1/2 and Fyn Kinase Through a Full Activation of Cloned Human 5-HT6 Receptors. Eur J Pharmacol. 2011 Jul 1;661(1-3):8-14. [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. 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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