Product Data Sheet

(rel)-AR234960

Catalog No. A24159

main product photo
(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.
Chemical Information
Catalog NumA24159
M. Wt555.62
FormulaC27H30FN5O5S
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.1408311-94-3
Synonyms
SMILESO=S(N1C[C@@H](CN2CCN(C3=NC=CC=C3)CC2)[C@H](C4=CC=CC(F)=C4)C1)(C5=CC=C([N+]([O-])=O)C=C5OC)=O
Biological Activity
Description(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.
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