The estrogen-related receptor α (ERRα) is an orphan nuclear receptor that can be regulated by peroxisome proliferator-activated receptor γ coactivator-1 (PGC-1). XCT790 is a selective inverse agonist for ERRα with an IC50 value of 0.37 μM, but displays no activity against ERRγ and estrogen receptors ERα and ERβ[3]. XCT-790 at 5 – 20 μM reduced the viability of HepG2 and R-HepG2 cells in a dose-dependent manner. The treatment of HepG2 and R-HepG2 cells with XCT-790 (10 μM) for 24 h reduced the protein levels of ERRα and decreased mitochondrial masses as compared to the DMSO-treated control group[4]. In mice inoculated with H295R adrenocortical cancer cells, the administration of XCT790 (2.5 mg/kg) for 21 days decreased H295R cell proliferation and suppressed tumor growth compared to the vehicle-treated group[5].
作用机制
XCT790 is a thiadiazoleacrylamide that functions as a potent inverse agonist of ERRα[3].
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