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:

alpha2A

Uniprot Number:

P08913

Protein Aliases:

alpha-2AAR subtype C10| alpha-2A-adrenergic receptor

Gene Name:

ADRA2A

Gene ID:

150

Gene Aliases:

ADRA2R|ADRAR

Organism:

Human

Construct Details:

Recombinant

Cell Type:

Chem-1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Activator:

Epinephrine Bitartrate

Test Concentration / Dose:

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

Test Sample Requirements:

Minimum for 1) Screen: 70 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

20179

Name

Clonidine

Measurement

5.67nM - EC50

PubChem ID

5815

Name

Epinephrine Bitartrate

Measurement

0.81nM - EC50

PubChem ID

66259

Name

Oxymetazoline hydrochloride

Measurement

4.83nM - EC50

PubChem ID

2435

Name

UK 14,304

Measurement

0.377nM - EC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

Adrenergic a2A receptor agonist may cause bradycardia and hypotension, inhibit insulin secretion resulting in hyperglycemia; antagonist may cause hypertension and exacerbate heart failure

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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