E-2508 free base
E-2508 free base is an orally active and highly selective corticotropin-releasing factor type 1 receptor (CRF1) antagonist with anxiolytic effects (Ki=11 nM). E-2508 free base blocks CRF-induced cAMP accumulation via CRF1 receptor inhibition. E-2508 free base is promising for research of stress-related psychiatric disorders, such as anxiety and depression.
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- CAS No.: 685885-75-0
- 화학식: C29H39N3O4
- 분자량:493.64
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
23 nM
Compound: 24r
|
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
|
[PMID: 22587443] |
| HEK293 | IC50 |
50 nM
Compound: 24r
|
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
|
[PMID: 22587443] |
Chemical Information
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CAS No. 685885-75-0
-
분자량 493.64
-
화학식 C29H39N3O4
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SMILES
CCC1=NN2C(C3=C(C=C(C=C3OC)COC)OC)=CC=CC2=C1N(CC4CCOCC4)CC5CC5
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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)