YM-254890

YM-254890 is cyclic depsipeptide originally isolated from Chromobacterium and an inhibitor of Galphaq/11. It inhibits Galphaq/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 Galphai-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 (Cay-90010, Cay-90010.1, Cay-10006607), or U-46619 (Cay-16450) in isolated human platelet-rich plasma (IC50s = 0.39, 0.15, 0.71, 0.25, and 0.34 µM, respectively). 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.Formal Name: N-acetyl-L-threonyl-(alphaR)-alpha-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-L-threonine(7->1)-lactone. CAS Number: 568580-02-9. Molecular Formula: C46H69N7O15. Formula Weight: 960.1. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 10 mg/ml. SMILES: O=C(N[C@@H](C)C1=O)C(N(C)C([C@H](OC([C@@H](NC(C)=O)[C@H](OC([C@@]([C@@H](C)OC)([H])N(C)C([C@@]([C@@H](C(C)C)OC([C@H]([C@H](O)C(C)C)NC(C)=O)=O)([H])NC([C@@H](N1C)C)=O)=O)=O)C)=O)CC2=CC=CC=C2)=O)=C. InChi Code: InChI=1S/C46H69N7O15/c1-22(2)37(56)34(49-30(11)55)45(63)68-38(23(3)4)35-43(61)53(14)36(28(9)65-15)46(64)66-27(8)33(48-29(10)54)44(62)67-32(21-31-19-17-16-18-20-31)42(60)52(13)25(6)39(57)47-24(5)41(59)51(12)26(7)40(58)50-35/h16-20,22-24,26-28,32-38,56H,6,21H2,1-5,7-15H3,(H,47,57)(H,48,54)(H,49,55)(H,50,58)/t24-,26-,27+,28+,32+,33-,34-,35-,36-,37+,38+/m0/s1. InChi Key: QVYLWCAYZGFGNF-WBWCVGBTSA-N. Origin: Bacterium/Chromobacterium sp.