Biological Information

Background Information:

Insulin primary role is to maintain blood glucose levels in the normal range. Secretion of Insulin by pancreatic B cells is controlled by hormones, nutrients and neurotransmitters however the primary stimulus for insulin secretion is the beta-cell response to changes in ambient glucose. Insulin secretion is triggered by the elevation of ATP in the pancreatic b cells caused by glucose metabolism. This ATP/ADP ratio increase will close the KATP channel leading to cell membrane depolarization and increase in cytosolic Ca++.

No. of Assays on Panel:

2

Assays on Panel:

Family

Endocrine System

Name

Item

331500-0

Protein

Organism

Hamster

Assay Sub Type

Cell Based

Family

Endocrine System

Name

Item

331500-1

Protein

Organism

Hamster

Assay Sub Type

Cell Based

Family:

Endocrine System

Sub Family:

Insulin

Class:

Mediator Release

Organism:

Hamster

Construct Details:

Endogenous

Cell Type:

HIT-T15

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist & Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Hamster HIT-T15 cells are used. Test compound and/or vehicle is incubated with the cells (1 Χ 10^6 /ml) in glucose buffer of insulin kit for 90 minutes at 37°C. Test compound-induced increase of insulin by 50 percent or more (≥50%) relative to the 100 mM glucose response indicates possible agonist activity. Test compound-induced inhibition of 10 mM glucose increase of insulin by 50 percent or more (≥50%) indicates antagonist activity.

Incubation:

1.5 hr at 37°C

Control Inhibitor:

Somatostatin-14

Control Activator:

D-Glucose

Criteria For Significance:

≥ 50% Increase in insulin release relative to glucose response, ≥ 50% Inhibition of glucose-induced insulin release

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:

20 Business Days

Reference Compound Data

PubChem ID

4788

Name

Phloretin

Measurement

>10μM - IC50

PubChem ID

5793

Name

D-Glucose

Measurement

2700μM - EC50

PubChem ID

44291156

Name

Somatostatin-14

Measurement

0.00039μM - IC50

PubChem ID

Name

KCl

Measurement

20000μM - EC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Adverse / Beneficial Action:

Increase in systemic insulin will lower glucose and this in turn will turn down the insulin secretion from the pancreatic cells.

Additional Information

Brand:

Panlabs

Testing Location:

Taiwan - Taipei