LY2608204 (C007B-203320)

InformationLY2608204 LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.In vitroLY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. LY2608204 also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM.In vivoLY2608204 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 LY2608204 concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg LY2608204 dose. The in vivo blood brain barrier permeability of LY2608204 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.Cell Datacell lines：Gpx4−/−cellsConcentrations：Incubation Time：Powder Purity:≥97%. Specification: 10mM in DMSO Molecular Formula: C28H37N3O3S3 Molecular Weight: 559.81