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

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at 37°C

Control Inhibitor:

AH 6809

Control Activator:

PGE2 (50 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

329770690

Name

AH 6809

Measurement

3890nM - IC50

PubChem ID

24724400

Name

AH23848

Measurement

57000nM - 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

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