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.

No. of Assays on Panel:

2

Assays on Panel:

Family

GPCR

Name

Item

338440-0

Protein

FP

Organism

Human

Assay Sub Type

Cell Based

Family

GPCR

Name

Item

338440-1

Protein

FP

Organism

Human

Assay Sub Type

Cell Based

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:

Agonist & Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human recombinant FP 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 30 minutes at 37°C. Test compound-induced increase of fluorescence by 50 percent or more (≥50%) relative to the 1 μM Cloprostenol response indicates possible FP receptor agonist activity. Test compound-induced inhibition of 5 nM Cloprostenol-induced increase of fluorescence response by 50 percent or more (≥50%) indicates receptor antagonist activity.

Incubation:

30 min at 37°C

Control Inhibitor:

AL-8810

Control Activator:

Cloprostenol

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

PubChem ID

5280360

Name

Prostaglandin E2

Measurement

0.77μM - EC50

PubChem ID

5280363

Name

Dinoprost

Measurement

0.028μM - EC50

PubChem ID

5311053

Name

Cloprostenol

Measurement

0.0014μM - EC50

PubChem ID

5311238

Name

AL-8810

Measurement

4.9μM - IC50

PubChem ID

9961192

Name

L-161,982

Measurement

3.1μM - IC50

PubChem ID

15551229

Name

L-798106

Measurement

4.5μM - IC50

PubChem ID

91746214

Name

Iloprost

Measurement

2.4μM - EC50

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

RELATED SOLUTIONS

Item: 338440-0
Item: 338440-1
Item: 268510