Estrogen ERβ agonist / Potent estrogen ERβ receptor agonist. Displays a 70-fold selectivity over ERα, EC50 = 0.85 and 66 nM, respectively.1 Regulates expression of GluR1, 2 and 3 in rat hippocampus.2 Ameliorates portal hypertension in a carbon tetrachloride-induced liver cirrhosis rat model.3 Stimulates proliferation of androgen-independent prostate cancer cell line PC-3 via a novel pathway involving ERβ-mediated activation of β-catenin.4 A useful tool for elucidating the biological function of ERβ.5
Biochemicals & reagents
1428-67-7
Diarylpropionitrile
1) Meyers et al. (2001), Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues; J. Med. Chem., 44 4230 2) Waters et al. (2009), Estrogen receptor alpha and beta specific agonists regulate expression of synaptic proteins in rat hippocampus; Brain Res., 1290 1 3) Zhang et al. (2016), Role of estrogen receptor beta selective agonist in ameliorating portal hypertension in rats with CC14-induced liver cirrhosis; World J. Gastroenterol., 22 4484 4) Lombardi et al. (2016), Estrogen receptor beta (ERβ) mediates expression of β-catenin and proliferation in prostate cancer cell line PC-3; Mol. Cell. Endocrin. 430 12 5) Harrington et al. (2003), Activities of estrogen receptor alpha- and beta-selective ligands at diverse estrogen responsive gene sites mediating transactivation and transrepression; Mol. Cell. Endocrinol., 206 13
-20°C
TARGET: Transcription factor -- PATHWAY: Estrogen; Beta-catenin; Proliferation; Transcription -- RESEARCH AREA: Neuroscience; Immunology -- DISEASE AREA: Cancer; HypertensionMood disorders; Inflammation