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. The EP1 prostanoid receptor is activated by prostaglandin E2 (PGE2) and it is most highly expressed in Kidney, myometrium and GI smooth muscle.

Family:

GPCR

Sub Family:

Prostanoid

Class:

Class A

Protein Name:

EP1

Uniprot Number:

P34995

Protein Aliases:

PGE2 receptor EP1 subtype|Prostanoid EP1 receptor

Gene Name:

PTGER1

Gene ID:

5731

Gene Aliases:

EP1

Accession Number:

NM_000955

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):

1.5

Ligand Concentration:

1.5 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:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

119461

Name

AH 6809

Measurement

2000nM - iC50

PubChem ID

5280360

Name

Prostaglandin E2

Measurement

1.4nM - iC50

PubChem ID

5311035

Name

Butaprost

Measurement

20000nM - iC50

PubChem ID

9869652

Name

AH 23848

Measurement

10000nM - iC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Prostanoid EP1 receptors may play a role in pain, regulation of blood pressure and cancer.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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