FERb 033

Cat. No.: HY-103446: FAQs
Data Sheet Handling Instructions

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FERb 033 is a selective and potent ERβ agonist (K_i=7.1 nM, EC₅₀=4.8 nM). FERb 033 shows 62-fold selectivity over ERα.

For research use only. We do not sell to patients.

FERb 033 Chemical Structure

CAS No. : 1111084-78-6

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Purity & Documentation
References
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Description

FERb 033 is a selective and potent ERβ agonist (K_i=7.1 nM, EC₅₀=4.8 nM). FERb 033 shows 62-fold selectivity over ERα^[1].

IC₅₀ & Target^[1]

ERβ

4.8 nM (EC₅₀)

ERβ

7.1 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
HEC-1	EC₅₀	19 nM Compound: 3	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	[PMID: 19128016]
HEC-1	EC₅₀	4.8 nM Compound: 3	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	[PMID: 19128016]

In Vitro

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.

Cell Viability Assay^[2]

Cell Line:	HEK293 cells
Concentration:	0-100 μM
Incubation Time:
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.

Cell Viability Assay^[3]

Cell Line:	ASM cells
Concentration:	10 nM
Incubation Time:	2 hours
Result:	Tended to decrease histamine-elicited Ca²⁺ response in nonasthmatic human ASM cells but not significantly compared to the control.

Molecular Weight

281.67

Formula

C₁₃H₉ClFNO₃

CAS No.

1111084-78-6

SMILES

ClC1=C(C2=CC(F)=C(O)C=C2)C=CC(/C=N/O)=C1O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

FERb 033 Related Classifications

Endocrinology

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FERb 0331111084-78-6FERb033FERb-033Estrogen Receptor/ERRselectivityHEK293ASMInhibitorinhibitorinhibit

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