MRS1220

**MRS1220** is a highly potent and selective antagonist for the human A3 adenosine receptor (hA3AR), with Ki values reported around 0.59–0.65 nM for hA3, demonstrating marked selectivity over other adenosine receptor subtypes (Ki = 305 nM for rat A1 and Ki = 52 nM for rat A2A)[1][4][7][9]. This small molecule acts by competitively inhibiting the binding and function of endogenous adenosine at the A3 receptor, thereby blocking A3AR-mediated signaling[8]. MRS1220 is frequently utilized in molecular and pharmacological research to dissect the role of the A3 adenosine receptor in cancer, neuroinflammation, and cardiovascular disease models. It has shown the ability to counteract the effects of A3 agonists (e.g., 2-Cl-IB-MECA and IB-MECA) in cell-based and animal studies, including blocking anti-proliferative and anti-inflammatory activities[2][3][6]. In preclinical models, MRS1220 has demonstrated therapeutic promise, notably reducing glioblastoma tumor size and angiogenesis[4]. The compound is not approved for clinical use and is intended for research applications only.

Brand names

MRS1220MRS-1220MRS 1220

Other names

MRS 1220MRS1220MRS-1220