mrs2179

MRS2179 is a competitive P2Y1 receptor antagonist with a Kb value of 100 nM and exhibits no appreciable activity at P2Y2, P2Y4, or P2Y6 receptors at concentrations up to 30 µM, nor at P2Y12 and P2Y13 receptors. MRS2179 inhibits ADP-induced platelet shape change and platelet aggregation in vitro, with a pA2 value of 6.55, and prolongs bleeding time in rats and mice relative to control groups. The receptor selectivity profile of MRS2179 supports its application in research focused on purinergic signaling, platelet biology, thrombosis-related mechanisms, and P2Y1 receptor-mediated cellular responses.

competitive antagonist at P2Y1 receptors

MRS2179 tetrasodium hydrate, a competitive antagonist of the P2Y1 receptor, acts on the turkey P2Y1 receptor (Kb: 102 nM, pA2: 6.99) and exhibits an inhibitory effect on platelet aggregation. IC50: 1.15 μM), P2X3 (IC50: 12.9 μM), P2X2, P2X4, P2Y2, P2Y4 and P2Y6 receptors.

MRS 2179 (ammonium) is a selective and competitive antagonist of the P2Y1 receptor (P2Y1 receptor) with a KB value of 0.177 μM.