Globalagliatin (LY2608204) is a activator of glucokinase (GK) with EC50 of 42 nM. IC 50 value: 42 nM (EC50) Target: glucokinase in vitro: Globalagliatin activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. Globalagliatin also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM. in vivo: Globalagliatin decreases plasma glucose in a dose-dependent manner at both fasted and postprandial glucose levels. A maximal lowering of glucose AUC versus the untreated control group is observed with the high dose (30 mg/kg) and represents a 42% decrease. Interpolation of the data show that a 20% glucose AUC decrease occurs at an average Globalagliatin concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg Globalagliatin dose. The in vivo blood brain barrier permeability of Globalagliatin results in a mean brain/plasma ratio of 0.17 five minutes post-dose with a mean total brain level of 0.539 nmol/g.
Chemical Name:
(1R,2S)-2-cyclohexyl-1-(4-cyclopropylsulfonylphenyl)-N-[5-(2-pyrrolidin-1-ylethylsulfanyl)-1,3-thiazol-2-yl]cyclopropane-1-carboxamide
Carbohydrate Metabolism Inhibitors Related Products:
Lonidamine; Epalrestat; Acarbose; Voglibose