Biological Activity
High affinity and selective 5-HT6 agonist (Ki = 2.2 nM). Displays 60-fold selectivity over other 5-HT and monoamine receptors. Increases firing rate of 5-HT neurons. Modifies sleep and wakefulness profiles following direct injections into the dorsal raphe nucleus, in vivo. Orally bioavailable.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc
Technical Data
| M. Wt | 470.91 |
| Formula | C15H13ClN4O2S2.C2H2O4 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1883548-85-3 |
| PubChem ID | 121513871 |
| InChI Key | KAFVDFYVWBASDD-UHFFFAOYSA-N |
| Smiles | NCCC2=CN(S(C3=C(Cl)N=C4N3C=CS4)(=O)=O)C1=CC=CC=C12.O=C(O)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 47.09 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 470.91. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.12 mL | 10.62 mL | 21.24 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.25 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Brouard et al (2015) Pharmacological evidence for 5-HT6 receptor modulation of 5-HT neuron firing in Vivo. ACS Chem.Neurosci. 6 1241 PMID: 25837696
Cole et al (2007) Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT6 receptor agonist. J.Med.Chem. 50 5535 PMID: 17948978
Keywords: WAY 181187 oxalate, supplier, WAY181187, oxalate, [554403-49-5], High, affinity, and, selective, 5-HT6, agonists, activates, sleep, serotonin, receptors, serotonergic, 5-HT6, Receptors, 5-HT6, Receptors, Tocris Bioscience
