WAY-361789
WAY-361789 (SEN15924) is an orally active agonist for α7 nicotinic acetylcholine receptor (α7 nAChR) with an EC50 of 0.18 μM. WAY-361789 improves the cognitive function, exhibits potential in ameliorating Alzheimer’s Disease and schizophrenia.
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- CAS No.: 1040718-40-8
- Formule: C22H31N5O3
- Masse moléculaire:413.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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AChE |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
3 μM
Compound: 25, SEN15924, WAY-361789
|
Agonist activity at human alpha7 nAChR expressed in CHO cells by whole cell patch clamp assay
Agonist activity at human alpha7 nAChR expressed in CHO cells by whole cell patch clamp assay
|
[PMID: 22468936] |
| CHO | IC50 |
24.2 μM
Compound: 25, SEN15924, WAY-361789
|
Inhibition of human ERG expressed in CHO cells by IonWorks assay
Inhibition of human ERG expressed in CHO cells by IonWorks assay
|
[PMID: 22468936] |
| GH4-C1 | EC50 |
0.18 μM
Compound: 25, SEN15924, WAY-361789
|
Agonist activity at rat alpha7 nAChR expressed in GH4C1 cells assessed as calcium influx measured every 1 sec for 1 min followed by every 30 secs for 10 mins by FLIPR assay
Agonist activity at rat alpha7 nAChR expressed in GH4C1 cells assessed as calcium influx measured every 1 sec for 1 min followed by every 30 secs for 10 mins by FLIPR assay
|
[PMID: 22468936] |
| GH4-C1 | EC50 |
4.4 μM
Compound: 25, SEN15924, WAY-361789
|
Agonist activity at rat alpha7 nAChR expressed in GH4C1 cells by whole cell patch clamp assay
Agonist activity at rat alpha7 nAChR expressed in GH4C1 cells by whole cell patch clamp assay
|
[PMID: 22468936] |
| HEK293 | IC50 |
>30 μM
Compound: 25, SEN15924, WAY-361789
|
Antagonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as inhibition of m-chlorophenylbiguanide-induced calcium influx measured every 1 sec for 1 min followed by every 3 secs for 3 mins by FLIPR assay
Antagonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as inhibition of m-chlorophenylbiguanide-induced calcium influx measured every 1 sec for 1 min followed by every 3 secs for 3 mins by FLIPR assay
|
[PMID: 22468936] |
| SH-SY5Y | IC50 |
>30 μM
Compound: 25, SEN15924, WAY-361789
|
Antagonist activity at human alpha3 receptor in SH-SY5Y cells assessed as inhibition of epibatidine-induced membrane potential measured every 1 sec for 1 min followed by every 3 secs for 3 mins by FLIPR assay
Antagonist activity at human alpha3 receptor in SH-SY5Y cells assessed as inhibition of epibatidine-induced membrane potential measured every 1 sec for 1 min followed by every 3 secs for 3 mins by FLIPR assay
|
[PMID: 22468936] |
| TE-671 | IC50 |
>30 μM
Compound: 25, SEN15924, WAY-361789
|
Antagonist activity at alpha1beta1deltagamma receptor in human TE671 cells assessed as inhibition of epibatidine-induced membrane potential measured every 1 sec for 1 min followed by every 3 secs for 3 mins by FLIPR assay
Antagonist activity at alpha1beta1deltagamma receptor in human TE671 cells assessed as inhibition of epibatidine-induced membrane potential measured every 1 sec for 1 min followed by every 3 secs for 3 mins by FLIPR assay
|
[PMID: 22468936] |
Chemical Information
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CAS No. 1040718-40-8
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Masse moléculaire 413.51
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Formule C22H31N5O3
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SMILES
O=C(NC1=NNC(C2=CC=C(OC)C=C2)=C1)CCCCN3CCN(C(C)=O)CCC3
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Synonyms
SEN15924
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Zanaletti R, et al. Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide (SEN15924, WAY-361789). J Med Chem. 2012 May 24;55(10):4806-23. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)