Biological Information

Background Information:

Chemokine 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. Chemokine receptors are primarily distributed on cells involved in immune and inflammatory function. Chemokine CXCR3 (CXC Chemokine Receptor 3) regulate leukocyte trafficking, integrin activation, cytoskeletal changes and chemotactic migration. CXCR3 is highly expressed in T cells.

PathHunter Activated GPCR Internalization cell lines are engineered to co-express an untagged GPCR, Enzyme Acceptor (EA) tagged β-Arrestin, and a ProLink™ (PK) tag localized to the endosomes. Activation of the GPCR induces β-Arrestin recruitment, followed by internalization of the Receptor/Arrestin-EA complex in PK-tagged endosomes. This forces complementation of the two β-galactosidase enzyme fragments (EA and PK), forming functional enzyme that hydrolyzes substrate to generate a chemiluminescent signal.

Family:

GPCR

Sub Family:

Chemokine

Class:

Class A

Coupling:

Gi/Go

Protein Name:

CXCR3

Uniprot Number:

P49682

Protein Aliases:

CXCR-3|CKR-L2|G protein-coupled receptor 9|Interferon-inducible protein 10 receptor|IP-10 receptor|CD antigen CD183

Gene Name:

CXCR3

Gene ID:

2833

Gene Aliases:

CKR-L2|CMKAR3|IP10-R|MigR|CD183

Accession Number:

AY242128

Organism:

Human

Cell Type:

U2OS

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

β-Arrestin Isoform:

β-Arrestin-2

Testing Information

Control Activator:

CXCL11/ ITAC

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:

CXCR3 has been associated with multiples diseases including diabetes, myasthenia gravis, multiple sclerosis, atherosclerosis and autoimmune diseases.

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA