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

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I][Sar1,Ile8]-AT-II

Ligand Kd (nM):

0.05

Ligand Concentration:

0.05 nM

Non Specific:

10 µM Angiotensin-II

Incubation:

120 min at 37°C

Control Inhibitor:

Saralasin

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

172198

Name

Angiotensin II

Measurement

3nM - IC50

PubChem ID

4673492

Name

ZD-7155

Measurement

0.5nM - IC50

PubChem ID

5311345

Name

PD123319

Measurement

- IC50

PubChem ID

6324663

Name

Saralasin

Measurement

0.63nM - 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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