(R)-DPN
(R)-DPN (compound 3) is a selective ERβ ligand with EC50s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC50s of 286, 205 nM, respectively.
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- CAS 番号: 524047-78-7
- 分子式: C15H13NO2
- 分子量:239.27
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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
|
ERα 2.9 nM (EC50) |
ERβ 0.8 nM (EC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEC-1 | EC50 |
286 nM
Compound: 3, R-DPN
|
Agonist activity at human ERalpha expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay
Agonist activity at human ERalpha expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay
|
[PMID: 22122563] |
| HEC-1 | EC50 |
3.2 nM
Compound: 3, R-DPN
|
Agonist activity at human ERbeta expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay
Agonist activity at human ERbeta expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay
|
[PMID: 22122563] |
| U2OS | EC50 |
205 nM
Compound: 3, R-DPN
|
Agonist activity at human ERalpha expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay
Agonist activity at human ERalpha expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay
|
[PMID: 22122563] |
| U2OS | EC50 |
3.4 nM
Compound: 3, R-DPN
|
Agonist activity at human ERbeta expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay
Agonist activity at human ERbeta expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay
|
[PMID: 22122563] |
化学情報
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CAS 番号 524047-78-7
-
分子量 239.27
-
分子式 C15H13NO2
-
SMILES
N#C[C@@H](C(C=C1)=CC=C1O)CC(C=C2)=CC=C2O
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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)