| Name | Globalagliatin |
| Description | Globalagliatin (LY2608204) has been used in trials studying the treatment of Diabetes Mellitus, Type 2. |
| In vitro | Under fasting and postprandial glucose conditions, LY2608204 demonstrated a dose-dependent reduction in blood glucose levels. Compared to the control group, the administration of a high dose of 30 mg/kg of the drug resulted in a maximum glucose-lowering effect of 42% on the glucose AUC. Interpolation analysis revealed that a 20% reduction in the glucose AUC occurred at an average LY2608204 concentration of 99 ng/mL (179 nM) in the plasma, equivalent to a dose of 6.9 mg/kg of LY2608204. The in vivo blood-brain barrier permeability of LY2608204 led to an average brain/plasma ratio of 0.17 and an average total brain level of 0.539 nmol/g, within 5 minutes. |
| In vivo | LY2608204 acts on rat insulinoma INS1-E cells, stimulating glucose metabolism with an EC50 of 579 nM. It activates glucokinase, presenting an EC50 of 42 nM in the presence of 10 mM glucose, demonstrating a concentration-dependent activation at lower glucose concentrations. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 33 mg/mL (58.9 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 103 mg/mL (184 mM)
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| Keywords | Hexokinase IV | Inhibitor | LY 2608204 | Hexokinase D | LY-2608204 | Globalagliatin | inhibit | Glucokinase |
| Inhibitors Related | ARRY-403 | ML251 | PFK-015 | 3PO | PFKFB3-IN-2 | Oxfendazole | AZ PFKFB3 26 | AMG-1694 | PFK-158 | Dorzagliatin | (1S,2R)-Globalagliatin | PF-04937319 |
| Related Compound Libraries | Glycometabolism Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | Drug Repurposing Compound Library | NO PAINS Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |
United States
