A-127722
A-127722 is A 2, 4-dialarylpyrrolidine-3-carboxylic acid ETA selective endothelin receptor (ET receptor) antagonist with IC50 value of 0.36 nM.
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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: 195704-72-4
- 分子式: C29H38N2O6
- 分子量:510.62
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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
製品説明
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.055 nM
Compound: 5; ABT-627; Xinlay
|
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
|
[PMID: 27266371] |
| MMQ | IC50 |
0.04 nM
Compound: 17v
|
Inhibition of phosphoinositol hydrolysis of MMQ cells.
Inhibition of phosphoinositol hydrolysis of MMQ cells.
|
[PMID: 8676339] |
| MMQ | IC50 |
0.31 nM
Compound: 17v
|
Inhibitory activity against the Endothelin A receptor of rat MMQ cells
Inhibitory activity against the Endothelin A receptor of rat MMQ cells
|
[PMID: 8676339] |
| MMQ | IC50 |
0.36 nM
Compound: 1
|
Binding affinity against Endothelin A receptor in MMQ cells in rat
Binding affinity against Endothelin A receptor in MMQ cells in rat
|
[PMID: 11689084] |
| Pituitary gland cell | IC50 |
0.4 nM
Compound: 13
|
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
|
[PMID: 9022798] |
化学情報
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CAS 番号 195704-72-4
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分子量 510.62
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分子式 C29H38N2O6
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SMILES
O=C([C@H]1[C@H](C2=CC=C(OC)C=C2)N(CC(N(CCCC)CCCC)=O)C[C@@H]1C3=CC=C(OCO4)C4=C3)O
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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.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)