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Globalagliatin

Catalog No. T3104   CAS 1234703-40-2
Synonyms: LY2608204

Globalagliatin (LY2608204) has been used in trials studying the treatment of Diabetes Mellitus, Type 2.

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Globalagliatin Chemical Structure
Globalagliatin, CAS 1234703-40-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 66.00
5 mg In stock $ 158.00
10 mg In stock $ 233.00
25 mg In stock $ 393.00
50 mg In stock $ 585.00
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Purity: 99.41%
ee: 100%
Purity: 98.26%
ee: 99.64%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 33 mg/mL (58.9 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 103 mg/mL (184 mM)

TargetMolReferences and Literature

1. Gupta, M., & Vadde, R. (2019). Insights into the structure–function relationship of both wild and mutant zinc transporter ZnT8 in human: a computational structural biology approach. Journal Of Biomolecular Structure And Dynamics, 1-15. doi: 10.1080/07391102.2019.1567391

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Clinical Compound Library Kinase Inhibitor Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max Glycometabolism Compound Library Bioactive Compound Library

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Keywords

Globalagliatin 1234703-40-2 Metabolism Glucokinase Hexokinase IV Inhibitor LY 2608204 Hexokinase D LY-2608204 inhibit LY2608204 inhibitor

 

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