EP4 Human Prostanoid GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
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., ductus arteriosus, kidney, lymphocytes, mononuclear cells, etc.). EP4 receptor agonism may mediate angiogenesis, vasorelaxation and bronchoprotective effects. EP4 receptor antagonism may be useful in the treatment of inflammation such as arthritis.
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
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
HEK293
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant prostanoid EP4 receptors expressed in HEK293 cells are used. Test compound or vehicle is incubated with the cells in incubation buffer for 5 minutes at 37 C. The reaction is evaluated for cAMP levels by TR-FRET. Test compound-induced increase of cAMP production by 50 percent or more (≥50%) relative to the 10 μM PGE2 response indicates possible EP4 receptor agonist activity. Test compound-induced inhibition of 20 nM PGE2-induced response in cAMP levels by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
5 min at 37°C
Control Inhibitor:
GW-627368
Criteria For Significance:
≥ 50% Inhibition of PGE2-induced cAMP increase
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:
Inflammation/Allergy
Adverse / Beneficial Action:
The EP4 receptor agonism plays a role in digestion, kidney reabsorption, uterine contraction, presynaptic inhibition of neurotransmitter release and potentiates platelet aggregation.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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