Biological Information

Background Information:

APJ (apelin) belongs to the superfamily of seven transmembrane G-protein-coupled receptors, which 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. APJ receptors are found in the lung, heart, and hypothalamic region.

Family:

GPCR

Sub Family:

Apelin

Class:

Class A

Protein Name:

APJ

Uniprot Number:

P35414

Protein Aliases:

APJ (apelin) receptor

Gene Name:

APLNR

Gene ID:

187

Gene Aliases:

FLJ90771|APJ|APJR

Accession Number:

NM_005161

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I](Glp65,Nle75,Tyr77)-apelin-13

Ligand Kd (nM):

0.06

Ligand Concentration:

0.03 nM

Non Specific:

1 µM Apelin-13

Incubation:

120 min at RT

Control Inhibitor:

apelin-13,TFA

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:

15 Business Days

Reference Compound Data

PubChem ID

16130451

Name

Apelin-36

Measurement

0.1nM - IC50

PubChem ID

Name

apelin-13,TFA

Measurement

0.2nM - IC50

PubChem ID

Name

[Pyr1]-apelin-13

Measurement

0.64nM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Adverse / Beneficial Action:

APJ receptors agonism may cause hypotension and protection against HIV cell entry.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 2844
Item: 2850
Item: G146
Item: P22-p