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 FP is a member of the prostaglandin series which are derived de novo from arachidonic acid and constitute the most abundant of the naturally occurring prostanoids. FP receptors are considered to be involved in smooth muscle contraction such as the uterus, vasculature, gastrointestinal tract, etc.
Family:
GPCR
Sub Family:
Prostanoid
Class:
Class A
Protein Name:
FP
Uniprot Number:
P43088
Protein Aliases:
PGF2-alpha receptor|Prostanoid FP receptor
Gene Name:
PTGFR
Gene ID:
5737
Gene Aliases:
FP
Accession Number:
NM_000959
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]PGF2alpha
Ligand Kd (nM):
3.83
Ligand Concentration:
2 nM
Non Specific:
10 µM Cloprostenol
Incubation:
60 min at RT
Control Inhibitor:
dinoprost
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
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Adverse / Beneficial Action:
FP receptor agonism may be useful in the treatment of ocular hypertension but may also be involved in untoward effects such as ocular hyperemia, cystoid macular edema, irishyperpigmentation or melanogenesis, excessive bone deposition, andpremature labor.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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