AT1 Human Angiotensin GPCR Cell Based Agonist & Antagonist IP1 LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
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.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
AT1 Human Angiotensin GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
302610-0
Protein
AT1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
AT1 Human Angiotensin GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item
302610-1
Protein
AT1
Organism
Human
Assay Sub Type
Cell Based
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:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant angiotensin AT1 receptors expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (1 x 10^6 /ml) in stimulation buffer of IP1 Tb kit for 30 minutes at 37°C. Test compound-induced increase of IP1 by 50 percent or more (≥50%) relative to the 0.3 μM angiotensin II response indicates possible AT1 receptor agonist activity. Test compound-induced inhibition of 1 nM angiotensin II-induced increase of IP1 response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
30 min at 37°C
Control Inhibitor:
144701-48-4
Control Activator:
Angiotensin II
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
Clinical Relevance
Therapeutic Area:
Cardiovascular
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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