IC50: N/A

DY131 is an agonist ligand for estrogen-related receptors ERRβ/γ. Estrogen receptor-related receptors (ERR) are orphan nuclear receptors constitutively activated without estrogen binding. ERRs may be involved in similar ER-mediated regulatory pathways and modulate estrogen responsiveness in certain target cells. The ERR subtypes, ERRβ/γ, are coexpressed in normal human prostatic epithelial cells and exhibit reduced expression in many prostate cancer cell lines.

In vitro: DY131 was evaluated for its selectivity and efficacy in modulating the transcriptional activity of ERRα/β/γ and ERβ/γ. CV-1 cells were transfected with reporter constructs or expression vectors and the fold activation of the reporter construct was determined at different concentrations of DY131. DY131 was found to be not able to activate the reporter construct or ERRα at any of the tested concentrations. In contrast, DY131 led to three- to fourfold activation of ERRβ at concentrations of 10-30 μM. Activity on ERRγ was more pronounced with five-fold activation at 3 μM and maximal 6.6-fold activity observed at 30 μM. Thus, DY131 was an selective ERRβ/γ ligand displaying preferential selectivity for ERRγ at lower concentrations [1].

In vivo: Currently, there is no animal in vivo data available for DY131 and its analogs.

Clinical trial: So far, no clinical study has been reported for DY131 and its analogs.

Reference:[1] Yu DD,Forman BM.  Identification of an agonist ligand for estrogen-related receptors ERRbeta/gamma. Bioorg Med Chem Lett.2005 Mar 1;15(5):1311-3.