851884-87-2

6-[[3-[(1S)-2-Methoxy-1-methylethoxy]-5-[(1S)-1-methyl-2-phenylethoxy]benzoyl]amino]-3-pyridinecarboxylic Acid, is one of the glucokinase activator derivatives. GKAs activate GK via binding to an allosteric site of the enzyme. They increase glucose-stimulated insulin secretion and decrease blood glucose levels. Also, glucokinase activator GKA50 is shown to be able to promote proliferation by increasing the cell volume and thus, preventing apoptosis in rat pancreatic insulinoma-1 beta cell.

GKA50 is a specific activator of glucokinase (EC50 = 0.03 μM). In mouse MIN6 insulin-secreting cells and r at pancreatic islet cellsGKA50 elicits a leftward shift in response to sub-maximal glucose concentrations as measured by insulin secretion and elevation of intracellular calcium levels.

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