YM-254890大环环肽，生物碱，链霉素代谢物主打

YM-254890 is cyclic depsipeptide originally isolated from Chromobacterium and an inhibitor of Gαq/11.1 It inhibits Gαq/11-mediated intracellular calcium mobilization induced by 2MeSADP or methacholine in C6-15 cells expressing the purinergic P2Y1 receptor (IC50 = 0.15 µM) and in CHO cells expressing M1 muscarinic acetylcholine receptors (IC50 = 0.15 µM), respectively, but has no effect on Gαi-mediated calcium mobilization induced by fMLP in HL-60 cells (IC50 = >10 µM). YM-254890 inhibits platelet aggregation induced by ADP, collagen, thrombin receptor agonist peptide (TRAP), arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), or U-46619 (Item No. 16450) in isolated human platelet-rich plasma (IC50s = 0.39, 0.15, 0.71, 0.25, and 0.34 µM, respectively).2 It reduces shear stress-induced thrombus formation in isolated human whole blood. YM-254890 (1, 3, and 10 µg/kg) reduces platelet thrombus formation in a cynomolgus monkey model of femoral artery thrombosis