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:

Full Length, Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

60 min at 37°C

Control Activator:

17-PGE₂

Criteria For Significance:

≥ 50% increase in IP-one relative to 17-PGE2 response, ≥ 50% inhibition of 17-PGE2-induced response

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

PubChem ID

5280360

Name

Prostaglandin E2

Measurement

0.0083μM - EC50

PubChem ID

5280363

Name

Dinoprost

Measurement

1.1μM - EC50

PubChem ID

5312153

Name

Sulprostone

Measurement

0.15μM - EC50

PubChem ID

91746214

Name

Iloprost

Measurement

0.055μM - EC50

PubChem ID

Name

17-PGE2

Measurement

0.0027μM - EC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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