Description
A cyclic depsipeptide Gαq/11 inhibitor; 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; inhibits ADP-, collagen-, TRAP-, arachidonic acid-, or U46619-induced platelet aggregation in isolated human platelet-rich plasma (IC50s = 0.39, 0.15, 0.71, 0.25, and 0.34 µM, respectively); reduces shear stress-induced thrombus formation in isolated human whole blood; reduces platelet thrombus formation in a cynomolgus monkey model of femoral artery thrombosis at 1, 3, and 10 µg/kg
Formal name: N-acetyl-L-threonyl-(αR)-α-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
Synonyms:
Molecular weight: 960.1
CAS: 568580-02-9
Purity: ≥95%
Formulation: A solid
