FERb 033
FERb 033 is a selective and potent ERβ agonist (Ki=7.1 nM, EC50=4.8 nM). FERb 033 shows 62-fold selectivity over ERα.
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- No. CAS: 1111084-78-6
- Fòrmula: C13H9ClFNO3
- Peso molecular:281.67
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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ERβ 4.8 nM (EC50) |
ERβ 7.1 nM (Ki) |
ERα 19 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEC-1 | EC50 |
19 nM
Compound: 3
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Agonist activity at full-length human estrogen receptor alpha expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
Agonist activity at full-length human estrogen receptor alpha expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
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[PMID: 19128016] |
| HEC-1 | EC50 |
4.8 nM
Compound: 3
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Agonist activity at full-length human estrogen receptor beta expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
Agonist activity at full-length human estrogen receptor beta expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
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[PMID: 19128016] |
FERb 033 (0-100 μM) shows specificity on full-length of estrogen receptor (ESR) in transactivation[2].
FERb 033 (10 nM, 2 h) treatment mildly decreases Ca2+ response in airway smooth muscle (ASM) cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:0-100 μM
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Incubation Time:
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Result:Induced transcriptional activity via full-length receptor on ERE with EC50 values of 0.253 and 0.053 μM for ESR1 and ESR2, respectively.
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Cell Line:ASM cells
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Concentration:10 nM
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Incubation Time:2 hours
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Result:Tended to decrease histamine-elicited Ca2+ response in nonasthmatic human ASM cells but not significantly compared to the control.
Chemical Information
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No. CAS 1111084-78-6
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Peso molecular 281.67
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Fòrmula C13H9ClFNO3
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SMILES
ClC1=C(C2=CC(F)=C(O)C=C2)C=CC(/C=N/O)=C1O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Filippo Minutolo, et al. Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta. J Med Chem. 2009 Feb 12;52(3):858-67. [Content Brief]
[2]. Satomi Kohno, et al. Estrogen receptor 1 (ESR1; ERα), not ESR2 (ERβ), modulates estrogen-induced sex reversal in the American alligator, a species with temperature-dependent sex determination. Endocrinology. 2015 May;156(5):1887-99. [Content Brief]
[3]. Sangeeta Bhallamudi, et al. Estrogen receptors differentially regulate intracellular calcium handling in human nonasthmatic and asthmatic airway smooth muscle cells. Am J Physiol Lung Cell Mol Physiol. 2020 Jan 1;318(1):L112-L124. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FERb 033 Related Classifications
HY-103446 Related Classifications
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