CAS 554403-49-5|WAY-181187
Introduction：Basic information about CAS 554403-49-5|WAY-181187, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | WAY-181187 | ||
|---|---|---|---|
| CAS Number | 554403-49-5 | Molecular Weight | 380.87200 |
| Density | / | Boiling Point | / |
| Molecular Formula | C15H13ClN4O2S2 | Melting Point | / |
| MSDS | / | Flash Point | / |
Names
| Name | 2-[1-(6-chloroimidazo[2,1-b][1,3]thiazol-5-yl)sulfonylindol-3-yl]ethanamine |
|---|---|
| Synonym | More Synonyms |
WAY-181187 BiologicalActivity
| 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]. |
|---|---|
| Related Catalog | Research Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor |
| Target | 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]. 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]. 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. |
| 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. [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. |
Chemical & Physical Properties
| Molecular Formula | C15H13ClN4O2S2 |
|---|---|
| Molecular Weight | 380.87200 |
| Exact Mass | 380.01700 |
| PSA | 119.01000 |
| LogP | 4.52320 |
| InChIKey | RYBOXBBYCVOYNO-UHFFFAOYSA-N |
| SMILES | NCCc1cn(S(=O)(=O)c2c(Cl)nc3sccn23)c2ccccc12 |
Synonyms
| way-181187 |
| unii-wxe3h7w295 |
