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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. |
| Synonyms | LY2608204 |
| Molecular Weight | 559.81 |
| Formula | C28H37N3O3S3 |
| Cas No. | 1234703-40-2 |
| Smiles | O=C(Nc1ncc(SCCN2CCCC2)s1)[C@@]1(C[C@H]1C1CCCCC1)c1ccc(cc1)S(=O)(=O)C1CC1 |
| Relative Density. | 1.35 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | 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. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7.15 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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