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. 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.

DiscoverX® Calcium cell lines overexpress naturally Gq coupled, wild type GPCRs and are designed to detect calcium mobilization in response to agonist stimulation of the receptor. Signal can be detected using the Calcium No WashPLUS Detection Kit.

Family:

GPCR

Sub Family:

Platelet-Activating Factor

Class:

Class A

Coupling:

Gi/Go & Gq

Protein Name:

PAF

Uniprot Number:

P25105

Protein Aliases:

PAFr

Gene Name:

PTAFR

Gene ID:

5724

Accession Number:

NM_000952.4

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Testing Information

Control Inhibitor:

ABT-491

Control Activator:

PAF

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

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:

USA - Fremont, CA