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

WAY-181187 (Synonyms: SAX-187)

Cat. No.: HY-14340 Purity: 98.05%
Handling Instructions

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.

WAY-181187 Chemical Structure

WAY-181187 Chemical Structure

CAS No. : 554403-49-5

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5 mg USD 330 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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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].

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

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].

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.

554403-49-5

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
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
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Keywords:

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

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Product Name:
WAY-181187
Cat. No.:
HY-14340
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