TA-0201
TA-0201 is a novel orally active, competitive, non-peptide endothelin receptor antagonist. TA-0201 antagonizes the specific binding of [125I]ET-1 to cloned human receptors of ETA and ETB with Ki values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1.
For research use only. We do not sell to patients.
- CAS No.: 169679-53-2
- Formula: C27H28BrN5O5S
- Molecular Weight:614.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
binding of [125I]ET-1 to cloned human receptors of ETA and ETB with Ki values of 15 pM and 41 nM, respectively[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A7R5 | IC50 |
0.015 nM
Compound: 26; TA0201
|
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cells
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cells
|
[PMID: 27321813] |
| CHO | IC50 |
0.4 nM
Compound: 2, T-0201
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Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
|
[PMID: 22862294] |
| CHO | IC50 |
12 nM
Compound: 2, T-0201
|
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
|
[PMID: 22862294] |
Chemical Information
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CAS No. 169679-53-2
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Molecular Weight 614.51
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Formula C27H28BrN5O5S
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SMILES
O=S(NC1=NC=NC(OCCOC2=NC=C(C=N2)Br)=C1C3=CC=C(C)C=C3)(C4=CC=C(C(C)(CO)C)C=C4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)