Globalagliatin

SKU: orb1304536

Description

Globalagliatin (LY2608204) is a glucokinase activator investigated as a potential therapeutic agent for Type 2 Diabetes. Research applications include in vitro enzymatic assays and in vivo studies in diabetic animal models to assess its glucose-lowering effects and mechanism of action.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1234703-40-2
• MW: 559.81
• Purity: 99.56% (May vary between batches)
• Formula: C₂₈H₃₇N₃O₃S₃
• SMILES: O=C(Nc1ncc(SCCN2CCCC2)s1)[C@@]1(C[C@H]1C1CCCCC1)c1ccc(cc1)S(=O)(=O)C1CC1
• Target: Glucokinase
• Solubility: Ethanol:33 mg/mL (58.95 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.15 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:103 mg/mL (183.99 mM)

Bioactivity

• Target IC50:
  GK:42 nM(EC50)
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Hexokinase IV, Hexokinase D, Globalagliatin, Glucokinase, glucokinase, LY 2608204, LY2608204, LY-2608204, Inhibitor, inhibit

Compound Identifiers

PubChem CID

46832368