Biological Information

Background Information:

Angiotensin receptors 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. Angiotensin AT1 receptors are expressed mainly in vascular smooth muscle, liver, kidney, heart, lung, adrenal cortex, pituitary and brain. AT1 receptor agonism may increase blood pressure, cell proliferation and migration and tubular Na+ resorption, while antagonists are therapeutically useful in the treatment of hypertension.

Family:

GPCR

Sub Family:

Angiotensin

Class:

Class A

Protein Name:

AT1

Uniprot Number:

P30556

Protein Aliases:

AT1BR|Angiotensin II type-1 receptor|AT1

Gene Name:

AGTR1

Gene ID:

185

Gene Aliases:

AT1|AT2R1|AGTR1A|AT2R1A|HAT1R|AG2S|AT2R1B|AT1B

Accession Number:

NM_009585

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:

30 min at 37°C

Control Inhibitor:

144701-48-4

Criteria For Significance:

≥ 50% increase in IP-one relative to angiotensin II response, ≥ 50% inhibition of angiotensin II-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

3961

Name

114798-26-4

Measurement

0.036μM - IC50

PubChem ID

65999

Name

144701-48-4

Measurement

0.026μM - IC50

PubChem ID

6324663

Name

Saralasin

Measurement

0.078μM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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