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:

Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Inhibitor:

Saralasin

Control Activator:

angiotensin-II (3 nM)

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

4673492

Name

ZD-7155

Measurement

0.95nM - IC50

PubChem ID

5311345

Name

PD123319

Measurement

- IC50

PubChem ID

6324663

Name

Saralasin

Measurement

1.6nM - IC50

PubChem ID

Name

[Sar1,Leu8]-AT-II

Measurement

2nM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

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.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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