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

PubChem ID

5280363

Name

Dinoprost

Measurement

2.02nM - IC50

PubChem ID

5311053

Name

Cloprostenol

Measurement

6nM - IC50

PubChem ID

5311221

Name

latanoprost

Measurement

2nM - IC50

PubChem ID

9869652

Name

AH 23848

Measurement

8000nM - IC50

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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