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.

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

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

20 min at 37°C

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

PubChem ID

3779

Name

Isoproterenol

Measurement

0.035μM - EC50

PubChem ID

9841972

Name

Brl-37344

Measurement

0.088μM - EC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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