EP1 Human Prostanoid GPCR Cell Based Agonist & Antagonist IP1 LeadHunter Assay - TW
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. The EP1 prostanoid receptor is activated by prostaglandin E2 (PGE2) and it is most highly expressed in Kidney, myometrium and GI smooth muscle.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
EP1 Human Prostanoid GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
338300-0
Protein
EP1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
EP1 Human Prostanoid GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item
338300-1
Protein
EP1
Organism
Human
Assay Sub Type
Cell Based
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 & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant EP1 receptors expressed in HEK293-EBNA1 cells are used. Test compound and/or vehicle is incubated with the cells (1 x 10^6 /ml) in stimulation buffer of IP1 Tb kit for 60 minutes at 37°C. Test compound-induced increase of IP1 by 50 percent or more (≥50%) relative to the 1 μM 17-PGE2 response indicates possible EP1 receptor agonist activity. Test compound-induced inhibition of 10 nM 17-PGE2-induced increase of IP1 response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
60 min at 37°C
Control Inhibitor:
SC-51322
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
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
EP1 Human Prostanoid GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item: 338300-0
EP1 Human Prostanoid GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item: 338300-1
EP1 Human Prostanoid GPCR Binding Agonist Radioligand LeadHunter Assay - TW
Item: 268110
Questions? Contact Us
You can easily get in touch with a Eurofins Discovery Expert or get help from our Customer Service team. Reach out with questions, or to discuss your specific discovery challenges.
