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

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Inhibitor:

SC-51322

Control Activator:

PGE2 (3 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 70 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

119461

Name

AH 6809

Measurement

587nM - IC50

PubChem ID

5311238

Name

AL-8810

Measurement

- IC50

PubChem ID

9869652

Name

AH 23848

Measurement

10300nM - IC50

PubChem ID

9933831

Name

SC-51322

Measurement

6.15nM - 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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