U-73122 U-73122;1-[6-[[(17B)-3-METHOXYESTRA-1,3,5(10)-TRIEN-17-YL]AMINO]HEXYL]-1H-PYRROLE-2,5-DIONE;1-[6-((17BETA-3-METHOXYESTRA-1,3,5(10)-TRIEN-17-YL)AMINO)HEXYL]-1H-PYRROLE-2,5-DIONE;U-73122 98%;1-[6-[((17 112648-68-7
U-73122 is an inhibitor of phospholipase C, phospholipase A2, and 5-LO (5-lipoxygenase).
IC50 value:
Target: phospholipase C/A2; 5-lipoxygenase
In neutrophils and human platelets, U-73122 inhibits agonist-induced phospholipase C (IC50=1.0-2.1 μM) activation. This compound affects the phospholipases by inhibiting the hydrolysis of PPI (phosphatidylinositol) to IP3 (inositol triphosphate), which in turn leads to a drop in cytosolic Ca2+. In SK-N-SH neuroblastoma cells, U-73122 inhibits agonist-induced down-regulation of muscarinic receptors. In addition, it is a useful tool to investigate receptor-mediated PI turnover in signal transduction. U-73122 is a potent inhibitor of human neutrophil adhesion to biological surfaces (IC50 = 50 nM) as well as adhesion-dependent granule exocytosis and oxidative burst. U-73122 is useful as a negative control for investigations of U-73122 phospholipase C antagonism and its cellular consequences.
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