Biological Information

Background Information:

Prostanoid 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. Prostanoid EP4 receptors are present in brain and many peripheral tissues (e.g., ileum>thymus>spleen>lung>heart>stomach).

Family:

GPCR

Sub Family:

Prostanoid

Class:

Class A

Protein Name:

EP4

Uniprot Number:

P35408

Protein Aliases:

PGE2 receptor EP4 subtype|Prostanoid EP4 receptor

Gene Name:

PTGER4

Gene ID:

5734

Gene Aliases:

EP4

Accession Number:

NM_000958

Organism:

Human

Construct Details:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

10 min at RT

Control Inhibitor:

GW 627368X

Control Activator:

PGE2 (30 nM)

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 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

5312130

Name

GW 627368X

Measurement

316nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

EP4 receptor agonism may exhibit intestinal cytoprotection, suppress hypermotility and colon cancer, reduce inflammatory activity (ulcerative colitis) and fever as well as increase wakefulness; use in the treatment of endotoxin shock and acute myocardial infarction have also been suggested. EP4 receptor antgonism may reduce intestinal mucosal and bronchopulmonary epithelial healing.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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