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:

alpha1A

Uniprot Number:

P35348

Protein Aliases:

Alpha-1A adrenoceptor|Alpha-1C adrenergic receptor|Alpha-adrenergic receptor 1c

Gene Name:

ADRA1A

Gene ID:

148

Gene Aliases:

ADRA1L1|ADRA1C

Accession Number:

NM_033303

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]prazosin

Ligand Kd (nM):

0.1

Ligand Concentration:

0.1 nM

Non Specific:

0.1 mM Epinephrine

Incubation:

60 min at RT

Control Inhibitor:

WB-4101

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 final 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:

2

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

2765

Name

Cirazoline

Measurement

350nM - IC50

PubChem ID

4893

Name

Prazosin

Measurement

0.4nM - IC50

PubChem ID

5685

Name

WB-4101

Measurement

0.36nM - IC50

PubChem ID

5816

Name

Epinephrine

Measurement

1200nM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

Adrenergic a1A receptor antagonism may result in hypotension as well as orthostatic hypotension and may be useful in the treatment of benign protatic hyperplasia.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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