MRS2578 is a potent, selective P2Y6 receptor antagonist with IC50 of 37 nM (human) and 101 nM (rat).
MRS2578 inhibits the response to 300 nM UDP at the rat P2Y6 receptor expressed in 1321N1 cells in a concentration-dependent manner, with IC50 values of 101 ± 27 nM and 98 ± 11 nM, respectively.
MRS2578 does not affect the UTP (100 nM)-induced responses of cells expressing P2Y2 and P2Y4 receptors as well as P2Y1 and P2Y11 receptor.
MRS2578 completely blocks the protection by UDP of cells undergoing TNFα-induced apoptosis at 1 uM.
MRS2578 bolcks ischemia/reperfusion injury in vivo in mouse skeletal muscle by P2Y6 receptor activation.
