568580-02-9
基本信息
物理化學(xué)性質(zhì)
常見問題列表
G αq/11 protein
YM-254890 inhibits platelet aggregation induced by ADP (2, 5 and 20 μM) in human platelet-rich plasma with IC 50 values of 0.37, 0.39 and 0.51 μM. ADP mediates platelet aggregation via two G protein-coupled receptors, P2Y 1 and P2Y 12 . The effect of YM-254890 on the P2Y 1 and P2Y 12 signal transduction pathways using C6-15 cells stably expressing the human P2Y 1 or P2Y 12 receptors is examined. Stimulation of P2Y 1 -C6-15 cells by 2MeSADP leads to increases in intracellular calcium mobilization. In this assay, YM-254890 inhibits the increase in [Ca 2+ ] i with an IC 50 value of 0.031 μM. In contrast, 2MeSADP-induced inhibition of forskolin-stimulated adenylyl cyclase activity in P2Y 12 -C6-15 cells is unaffected by YM-254890 at 40 μM.