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[1].

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Endocrinology

ERβ:4.8 nM (EC50)

ERβ:7.1 nM (Ki)

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]. 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.

[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.

[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.

[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.