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:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

30 min at 37°C

Control Activator:

CHEMBL109783

Criteria For Significance:

≥ 50% increase in IP-one relative to A61603 response, ≥ 50% Inhibition of A61603-induced response

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

2765

Name

Cirazoline

Measurement

0.082μM - EC50

PubChem ID

5709

Name

Xylometazoline

Measurement

0.066μM - EC50

PubChem ID

5816

Name

Epinephrine

Measurement

0.094μM - EC50

PubChem ID

4038180

Name

CHEMBL109783

Measurement

0.0037μM - EC50

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 prostatic hyperplasia.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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