| 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/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (7.15 mM), Sonication is recommended.
Ethanol : 33 mg/mL (58.95 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 103 mg/mL (183.99 mM), Sonication is recommended.
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| Keywords | LY-2608204 | LY 2608204 | Inhibitor | inhibit | Hexokinase IV | Hexokinase D | glucokinase | Globalagliatin |
| Inhibitors Related | Gcase activator 2 | ARRY-403 | ML251 | PFK-015 | PFKFB3-IN-2 | D-(-)-3-Phosphoglyceric acid disodium | Oxfendazole | AZ PFKFB3 26 | AMG-1694 | RO-28-1675 | Dorzagliatin | PF-04937319 |
| Related Compound Libraries | Glycometabolism Compound Library | Glycolysis Compound Library | Failed Clinical Trials Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | ReFRAME Related Library | Kinase Inhibitor Library | Drug Repurposing Compound Library | NO PAINS Compound Library | Metabolism Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |
United States
