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
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
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