FP Human Prostanoid GPCR Binding Agonist Radioligand LeadHunter Assay - TW

Item: 268510

Price: Login to View Pricing

Status: Available

ADD TO CART

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. 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 protanoids. 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:

Uniprot Number:

P43088

Protein Aliases:

PGF2-alpha receptor|Prostanoid FP receptor

Gene Name:

PTGFR

Gene ID:

5737

Gene Aliases:

Accession Number:

NM_000959

Organism:

Human

Construct Details:

Full Length, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human recombinant prostanoid FP receptors expressed in HEK293 cells are used in modified MES buffer pH 6.0. A 80 μg‡ aliquot is incubated with 1 nM [³H]PGF2α for 60 minutes at 25°C. Non-specific binding is estimated in the presence of 1 μM Cloprostenol. Membranes are filtered and washed, the filters are then counted to determine [³H]PGF2a specifically bound. Compounds are screened at 10 μM.
Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.

Ligand:

[³H] PGF2alpha

Ligand Kd (nM):

2.4

Ligand Concentration:

1 nM

Non Specific:

1 µM Cloprostenol

Incubation:

60 min at 25°C

Control Inhibitor:

Dinoprost

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Test Sample Requirements:

Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5280360

Name

Prostaglandin E2

Measurement

0.045μM - IC50

PubChem ID

5280363

Name

Dinoprost

Measurement

0.001μM - IC50

PubChem ID

5311053

Name

Cloprostenol

Measurement

0.0012μM - IC50

PubChem ID

91746214

Name

Iloprost

Measurement

0.48μM - 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:

Taiwan - Taipei