(rel)-AR234960 is a selective and competitive agonist of the G protein-coupled receptor MAS . (rel)-AR234960 binds to the MAS receptor to activate the downstream ERK1/2 signaling pathway, inducing the expression of connective tissue growth factor ( CTGF ) and its downstream collagen subtype genes (such as COL1A1, COL3A1). (rel)-AR234960 promotes collagen synthesis in cardiac fibroblasts through the MAS-ERK1/2-CTGF pathway and aggravates extracellular matrix remodeling. (rel)-AR234960's in vitro effect can be blocked by the MAS inverse agonist AR244555 and MEK1 inhibitor . (rel)-AR234960 regulates the expression of cardiac fibrosis-related genes and can be used in the study of heart failure.
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