Biological Information

Background Information:

Adrenoreceptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Adrenoreceptors are found in most peripheral tissue and within the central nervous system.

Family:

GPCR

Sub Family:

Adrenoceptor

Class:

Class A

Protein Name:

beta1

Uniprot Number:

P08588

Protein Aliases:

Beta-1 adrenoceptor

Gene Name:

ADRB1

Gene ID:

153

Accession Number:

NM_000684

Organism:

Human

Construct Details:

Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at RT

Control Inhibitor:

Atenolol

Control Activator:

isoproterenol (5 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL testing. 2) Dose Response: 90 µL of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

2249

Name

Atenolol

Measurement

284nM - IC50

PubChem ID

2685

Name

CGP-20712A

Measurement

5.26nM - IC50

PubChem ID

4946

Name

Propranolol

Measurement

18nM - IC50

PubChem ID

Name

ICI 118551

Measurement

1915nM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

Selective 1-adrenoceptor antagonism may be useful in the treatment of hypertension and stable angina; may also cause bradycardia.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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