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Globalagliatin (LY2608204) has been used in trials studying the treatment of Diabetes Mellitus, Type 2.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $32 | In Stock | |
2 mg | $45 | In Stock | |
5 mg | $73 | In Stock | |
10 mg | $98 | In Stock | |
1 mL x 10 mM (in DMSO) | $90 | In Stock |
Description | Globalagliatin (LY2608204) has been used in trials studying the treatment of Diabetes Mellitus, Type 2. |
Targets&IC50 | GK:42 nM(EC50) |
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. |
Alias | LY2608204 |
Molecular Weight | 559.81 |
Formula | C28H37N3O3S3 |
Cas No. | 1234703-40-2 |
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) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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