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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1040718-40-8
- 分子式: C22H31N5O3
- 分子量:413.51
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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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] |
化学情報
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CAS 番号 1040718-40-8
-
分子量 413.51
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分子式 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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別名
SEN15924
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)