(rel) -AR234960

(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[1][2].

Product Specifications

CAS Number

[1408311-94-3]

UNSPSC

12352005

Target

ERK

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/rel-ar234960.html

Purity

98.95

Solubility

DMSO : 25 mg/mL (ultrasonic; heat to 80°C)

Smiles

O=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

Molecular Formula

C27H30FN5O5S

Molecular Weight

555.62

References & Citations

[1]Chen Z, et al. Suppression of Skp2 contributes to sepsis-induced acute lung injury by enhancing ferroptosis through the ubiquitination of SLC3A2. Cell Mol Life Sci. 2024 Jul 30;81 (1) :325.|[2]Chatterjee A, et al. Connective tissue growth factor dependent collagen gene expression induced by MAS agonist AR234960 in human cardiac fibroblasts. PLoS One. 2017 Dec 29;12 (12) :e0190217.