Biological Information

Background Information:

GLP-1R (Glucagon-like peptide-1 (GLP-1) receptor), a G-protein coupled receptor coupling to a Gαs subunit, regulates two peptide-mediated biased agonisms, cAMP/calcium signaling and ERK activity. GLP-1R is widely expressed in many tissues and organs, such as the pancreas, stomach, duodenum, lung, and hypothalamus. Activated GLP-1R stimulates insulin secretion and reduces glucagon secretion in pancreatic cells. In the brain, GLP-1R signaling controls appetite to reduce food intake and regulates glucose homeostasis by decreasing hepatic production and muscle uptake. The endogenous agonist of GLP-1R, GLP-1, released from endocrine L-cells of the gut and the nucleus of the solitary tract, controls meal-related glycemic excursions. The beneficial effects of GLP-1R action on energy and glucose metabolism promote current GLP-1R agonist-based therapies for the treatment of diabetes and obesity.

Family:

GPCR

Sub Family:

Glucagon

Class:

Class A

Protein Name:

GLP-1R

Uniprot Number:

P43220

Protein Aliases:

GLP-1R|GLP-1 receptor|GLP-1-R

Gene Name:

GLP1R

Gene ID:

2740

Gene Aliases:

GLP-1R|glucagon like peptide 1 receptor

Accession Number:

NM_002062.2

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

Chem-1

Assay Information

Assay Type:

Functional

Assay Sub Type:

GTPgammaS

Functional Mode:

Agonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human recombinant GLP-1 receptors expressed in Chem-1 cells are used. Test compound and/or vehicle is preincubated with the 63 μg/mlǂ receptors and 1 μM GDP in modified HEPES buffer pH 7.4 for 20 minutes at RT; SPA beads are then added for another 60 minutes at 30℃. The reaction is initiated by 0.3 nM [35S]GTPgS for an additional 15-minute incubation period. Test compound-induced increase of [35S]GTPgS binding by 50 percent or more (≥50%) relative to 0.1 μM GLP-1 (7-36) response indicates possible GLP-1 receptor agonist activity.

Incubation:

15 min at 30°C

Control Activator:

GLP-1 (7-36)

Criteria For Significance:

≥ 50% Increase in bound [35S]GTPgammaS relative to GLP-1 (7-36) response

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

16133831

Name

GLP-1 (7-36)

Measurement

0.93nM - EC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Adverse / Beneficial Action:

Activated GLP-1R stimulates insulin secretion and reduces glucagon secretion in pancreatic cells. In the brain, GLP-1R signaling controls appetite to reduce food intake and regulates glucose homeostasis by decreasing hepatic production and muscle uptake. The endogenous agonist of GLP-1R, GLP-1, released from endocrine L-cells of the gut and the nucleus of the solitary tract, controls meal-related glycemic excursions. The beneficial effects of GLP-1R action on energy and glucose metabolism promot

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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