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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- CAS No.: 195704-72-4
- Formule: C29H38N2O6
- Masse moléculaire:510.62
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
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] |
Chemical Information
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CAS No. 195704-72-4
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Masse moléculaire 510.62
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Formule 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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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.
Protocole
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)