beta3 Human Adrenoceptor GPCR Cell Based Agonist & Antagonist cAMP LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
There are three known subtypes of b-adrenergic receptors, b1, b2, and b3, all of which are thought to couple primarily via Gsa to adenylyl cylase, leading to an increase in cAMP. The receptor subtypes differ primarily in their location: b1-adrenoceptors predominate in the heart, cerebral cortex, and the kidney. The major subtype in the lungs, cerebellum, uterus, skeletal muscle, and blood vessels is the b2-adrenoceptor. The b3-adrenoceptor has been detected in brain, stomach, and gall bladder but are expressed predominantly in white and brown adipose tissue (WAT and BAT, respectively) and selective agonists may be potentially useful as anti-obesity drugs.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
beta3 Human Adrenoceptor GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
Item
302200-0
Protein
beta3
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
beta3 Human Adrenoceptor GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
Item
302200-1
Protein
beta3
Organism
Human
Assay Sub Type
Cell Based
Family:
GPCR
Sub Family:
Adrenoceptor
Class:
Class A
Protein Name:
beta3
Uniprot Number:
P13945
Protein Aliases:
Beta-3 adrenoceptor
Gene Name:
ADRB3
Gene ID:
155
Accession Number:
NM_000025
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
HEK293
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:
Human recombinant adrenergic b3 receptors expressed in HEK-293 cells are used. Test compound and/or vehicle is incubated with the cells (1.25 x 10^5 cell/ml) in modified HBSS pH 7.4 buffer for 20 minutes at 37°C. The reaction is evaluated for cAMP levels by TR-FRET. Test compound-induced cAMP increase by 50 percent or more (≥50%) relative to the 1 µM Isoproterenol control response indicates possible adrenergic b3 receptor agonist activity. Test compound-induced inhibition of the 0.2 µM Isoproterenol-induced cAMP response by 50 percent or more (≥50%) indicates receptor antagonist activity. These same concentrations are concurrently applied to a separate group of treated cells and evaluated for possible compound-induced cytotoxicity only if significant inhibition of cAMP release is observed (Cat. #302300).
Incubation:
20 min at 37°C
Control Inhibitor:
S(-)-Propranolol
Control Activator:
Isoproterenol
Criteria For Significance:
≥50% Increase in cAMP relative to Isoproterenol response, ≥50% Inhibition of Isoproterenol-induced cAMP increase
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
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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