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:
Full Length, Recombinant
Cell Type:
HEK293
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Incubation:
30 min at 37°C
Control Inhibitor:
AL-8810
Criteria For Significance:
≥ 50% increase in IP-one relative to Cloprostenol response, ≥ 50% inhibition of Cloprostenol-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
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:
Taiwan - Taipei
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