PSN-GK1 is a potent activator of glucokinase (EC50: 0.13 μM).

PSN-GK1 exhibits an excellent pharmacokinetic profile, with high oral bioavailability, in the rat. PSN-GK1 can markedly reduce blood glucose which accompanied by a trend toward increased pancreatic insulin release. PSN-GK1 engenders potent antihyperglycemic effects in diabetic rodents without causing hypoglycemia [1]. At 5 mM glucose, PSN-GK1 activates glucokinase (4.3-fold, EC50: 130 nM), increases MIN6 insulin secretion (26-fold, EC50: 267 nM) and 2-DG hepatocytic uptake (3-fold, EC50: 1 μM). In C57Bl/6 mice, PSN-GK1 reduces blood glucose at 1 and 10 mg/kg (by mouth), but insulin is increased significantly at only the higher dose. In hyperinsulinaemic 10-mM glucose clamps, PSN-GK1 increases2-DG incorporation into liver glycogen sixfold [2].