[3H]-2-Deoxy-D-Glucose Rat Transporter Cell Based Agonist & Antagonist Uptake Assay, Panlabs
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Insulin, a hormone produced in the islets of Langerhans of the pancreas, regulates the metabolism of carbohydrates, fats, and starches in the body. It initiates its signal transduction cascade by activating the insulin receptor tyrosine kinase, leading to phosphorylation of phosphoprotein substrates, activation of PI3-kinase and stimulation of glucose transport. Phosphorylation of IRS-1, which binds to and activates PI3-kinase, is one mechanism by which insulin stimulates PI3-kinase to mediate glucose transport. More recently, it has been recognized that a separate PI3-kinase independent pathway is initiated by insulin stimulation, which must complement the PI3-kinase dependent pathway to achieve full GLUT4 translocation. Compounds, acting as insulin to increase glucose uptake, would be beneficial in the treatment of diabetes mellitus.
No. of Assays on Panel:
2
Assays on Panel:
Family
Transporter
Name
[3H]-2-Deoxy-D-Glucose Rat Transporter Cell Based Agonist Uptake Assay, Panlabs
Item
320020-0
Protein
Organism
Rat
Assay Sub Type
Cell Based
Family
Transporter
Name
[3H]-2-Deoxy-D-Glucose Rat Transporter Cell Based Antagonist Uptake Assay, Panlabs
Item
320020-1
Protein
Organism
Rat
Assay Sub Type
Cell Based
Family:
Transporter
Sub Family:
SLC2 / Glucose
Class:
SLC
Organism:
Rat
Construct Details:
Endogenous
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist & Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Differentiate rat L6 skeletal muscle cells are used. Test compound and/or vehicle is incubated with the cells in MEM-modified medium for 24 hours at 37°C 5% CO₂ incubator. After 24 hours, [³H]-2-Deoxy-D-glucose is added each well for 15 minutes incubation period. Test compound-induced increase of [³H]-2-Deoxy-D-glucose uptake by 50 percent or more (≥50%) relative to the 100 μg/ml insulin response indicates possible agonist activity. Test compound-induced inhibition of 10 μg/ml insulin-induced increase of [³H]-2-Deoxy-D-glucose uptake response by 50 percent or more (≥50%) indicates antagonist activity.
Incubation:
15 min at 37°C
Control Inhibitor:
LY294002
Control Activator:
Insulin
Criteria For Significance:
≥ 50% Increase in 2-DG uptake relative to insulin response, ≥ 50% Inhibition of insulin-induced 2-DG uptake
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
30 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
Panlabs
Testing Location:
Taiwan - Taipei
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Item: 243000
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