YM-254890 (C09-1185-584)

YM-254890 is a selective G αq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y 1 signal transduction pathway, with an IC 50 value below 0.6 μMIn VitroYM-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:P2Y1 Receptor. Specification: ≥95.0% Molecular Formula: C46H69N7O15 Molecular Weight: 960.08 PubChem CID: 9919454 Isomeric SMILES: C[C@@H]1[C@@H](C(=O)O[C@@H](C(=O)N(C(=C)C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)O1)[C@@H](C)OC)C)[C@@H](C(C)C)OC(=O)[C@H]([C@@H](C(C)C)O)NC(=O)C)C)C)C)C)CC2=CC=CC=C2)NC(=O)C