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). b2 adrenoceptors are mainly associated with causing relaxation of smooth muscle in a variety of tissues. Adrenergic b2 receptor agonism have been found useful in the treatment of bronchospasm but may facilitate cardiac arrest. Adrenergic b2 receptor antagonism may facilitate bronchospasm and impair exercise stress cardiovascular performance.

Family:

GPCR

Sub Family:

Adrenoceptor

Class:

Class A

Protein Name:

beta2

Uniprot Number:

P07550

Protein Aliases:

Beta-2 adrenoceptor

Gene Name:

ADRB2

Gene ID:

154

Gene Aliases:

ADRBR|BAR|B2AR

Accession Number:

NM_000024

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

20 min at 37°C

Control Inhibitor:

ICI-118,551

Criteria For Significance:

≥50% Increase in cAMP relative to procaterol response, ≥50% Inhibition of procaterol-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

Name

ICI-118,551

Measurement

0.008μM -

Clinical Relevance

Therapeutic Area:

Pulmonology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: 302150
Item: 302150-0
Item: 204110