MRS2500

MRS2500 is a synthetic, nucleotide-like small-molecule antagonist that is highly potent, selective, and stable at the purinergic P2Y1 receptor, a G protein–coupled receptor activated by ADP and expressed on platelets and vascular cells.[1][4][6] By competitively blocking P2Y1, MRS2500 prevents ADP-induced platelet shape change and aggregation, thereby exhibiting strong antithrombotic activity in vivo with relatively modest effects on bleeding time in animal models.[1][3][5] Crystallographic studies show that MRS2500 binds within the seven-transmembrane bundle of human P2Y1R close to the extracellular surface, where extensive interactions with charged and polar residues stabilize the receptor in an inactive conformation.[5][10] Initially developed in an academic/NIH setting as a pharmacological tool compound rather than a clinical drug, MRS2500 is widely used in preclinical research to probe P2Y1 biology, thrombosis, vascular inflammation, neuropathic pain, and other P2Y1-mediated processes.[1][5][7][11][12]

Other names

MRS 2500 tetraammonium saltMRS2500 tetraammonium saltMRS-2500 tetraammonium salt2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate(1R,2S)-4-[2-iodo-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol dihydrogen phosphate ester tetraammonium salt