(rel)-AR234960 is a selective and competitive agonist of the MAS G protein-coupled receptor (GPCR), known for its role in cardiovascular regulation. Upon binding to the MAS receptor, (rel)-AR234960 activates the ERK1/2 signaling cascade, leading to the upregulation of connective tissue growth factor (CTGF) and downstream collagen subtype genes, including COL1A1 and COL3A1.
This activation promotes collagen synthesis in cardiac fibroblasts via the MAS–ERK1/2–CTGF axis, contributing to extracellular matrix remodeling and the progression of cardiac fibrosis. The fibrotic effects of (rel)-AR234960 can be reversed by the MAS inverse agonist AR244555 or by inhibition of MEK1, a key upstream regulator of ERK1/2.
(rel)-AR234960 is a selective and competitive agonist of the MAS G protein-coupled receptor (GPCR), known for its role in cardiovascular regulation. Upon binding to the MAS receptor, (rel)-AR234960 activates the ERK1/2 signaling cascade, leading to the upregulation of connective tissue growth factor (CTGF) and downstream collagen subtype genes, including COL1A1 and COL3A1.
This activation promotes collagen synthesis in cardiac fibroblasts via the MAS–ERK1/2–CTGF axis, contributing to extracellular matrix remodeling and the progression of cardiac fibrosis. The fibrotic effects of (rel)-AR234960 can be reversed by the MAS inverse agonist AR244555 or by inhibition of MEK1, a key upstream regulator of ERK1/2.
Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 1 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
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