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.
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: 169679-53-2
- 分子式: C27H28BrN5O5S
- 分子量:614.51
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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
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
|
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
|
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] |
化学情報
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CAS 番号 169679-53-2
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分子量 614.51
-
分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)