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Globalagliatin
CAS No. : 1234703-40-2
Biological Activity：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.
Research Area：Metabolic Disease
Targets：Glucokinase
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Related Small Molecules:PF-04937319;Palmitelaidic Acid;Glucokinase activator 1;AZD1656;AMG-3969;RO-28-1675;IHVR-11029;Cadisegliatin;PSN-GK1;Glucokinase activator 3;PF-04991532;Dorzagliatin;AR453588 hydrochloride;GKA50 quarterhydrate;AMG-1694;Palmitelaidic acid-d13;BMS-820132;MK-0941 free base;AM-2394
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