MRS1754

MRS1754 is a potent and selective small molecule antagonist of the adenosine A2B receptor (A2BR). It was developed as a pharmacological research tool to investigate the physiological and pathological roles of the A2B receptor subtype, which is involved in inflammation, asthma, and cancer progression. In oncology research, MRS1754 has been used to study how A2BR signaling modulates intercellular adhesions and paracellular permeability, particularly in hypoxic microenvironments. Studies in endometrial carcinoma models have shown that antagonism of A2BR by MRS1754 can lead to the downregulation of junctional adhesion proteins like claudin-1 and claudin-2, potentially promoting cancer cell migration and invasion. MRS1754 exhibits high affinity for the human A2B receptor (Ki ≈ 2 nM) and demonstrates significant selectivity over other adenosine receptor subtypes (A1, A2A, and A3).

Other names

N-(4-cyanophenyl)-2-[4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-purin-8-yl)phenoxy]acetamide