EP2 Human Prostanoid GPCR Binding Agonist Radioligand LeadHunter Assay - FR

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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 EP2 receptors are present in brain and many peripheral tissues (e.g., lung, placenta, uterus, ileum, stomach, spleen, thymus, etc.).

Family:

GPCR

Sub Family:

Prostanoid

Class:

Class A

Protein Name:

EP2

Uniprot Number:

P43116

Protein Aliases:

PGE2 receptor EP2 subtype|Prostanoid EP2 receptor

Gene Name:

PTGER2

Gene ID:

5732

Gene Aliases:

EP2

Accession Number:

NM_000956

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]PGE2

Ligand Kd (nM):

Ligand Concentration:

3 nM

Non Specific:

10 µM PGE2

Incubation:

120 min at RT

Control Inhibitor:

Prostaglandin E2

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:

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

119461

Name

AH 6809

Measurement

900nM - IC50

PubChem ID

5280360

Name

Prostaglandin E2

Measurement

1.7nM - IC50

PubChem ID

5311035

Name

Butaprost

Measurement

3300nM - IC50

PubChem ID

44364273

Name

U-44069

Measurement

230nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

EP2 receptor agonism may reduce myometrial activity, bronchospasm and vasoconstriction as well as promote fever, increase gastrointestinal motility, renal nutriuresis and diuresis. EP2 receptor antagonism may be useful in the treatment of migraine but facilitate salt-sensitive hypertension.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault