Biological Information

Background Information:

PAF 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. PAF receptors are found in a diverse array of cells, including neutrophilic polymorphonuclear leukocytes (PMN), platelets, mast cells, monocytes/macrophages, vascular endothelial cells and lymphocytes. PAF receptor stimulation is involved in intracrine, autocrine, paracrine and juxtacrine cell activation.

Family:

GPCR

Sub Family:

Platelet-Activating Factor

Class:

Class A

Protein Name:

PAF

Uniprot Number:

P25105

Protein Aliases:

PAFr

Gene Name:

PTAFR

Gene ID:

5724

Accession Number:

NM_000952

Organism:

Human

Construct Details:

Recombinant

Cell Type:

Chem-1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Activator:

PAF (3 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 70 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

65889

Name

Apafant

Measurement

916nM - IC50

PubChem ID

107757

Name

CV-6209

Measurement

41nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

PAF receptor agonism may exacerbate inflammation, allergic asthma, atherosclerosis, psoriasis and neurotoxicity. PAF receptor antagonism may be useful as an adjunct in the treatment of hemorrhagic and septic shock; receptor antagonism may also impair memory.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 4300
Item: G291