Biological Information

Background Information:

CXCR4 (CXC Chemokine Receptor 4), also called fusin, is an alpha-chemokine receptor specific for stromal-derived-factor-1 (SDF-1 also called CXCL12), a molecule endowed with potent chemotactic activity for lymphocytes. It is highly expressed in brain and heart, and in white blood cells, vascular endothelial cells, umbilical cord endothelial cells, and several tumor cell lineages. This receptor is an HIV-1 fusion co-factor that allows HIV-1 invasion in diverse human cell types. CXCR4 is involved in organ vascularization, neuronal cell migration, and patterning of the central nervous system during development.

Family:

GPCR

Sub Family:

Chemokine

Class:

Class A

Protein Name:

CXCR4

Uniprot Number:

P61073

Protein Aliases:

CXCR-4|Fusin|Leukocyte-derived seven transmembrane domain receptor|LESTR|Pre-B-cell-derived chemokine receptor|PB-CKR|Stromal cell-derived factor 1 receptor|SDF-1 receptor|CD antigen CD184

Gene Name:

CXCR4

Gene ID:

7852

Gene Aliases:

LESTR|NPY3R|HM89|NPYY3R|D2S201E|fusin|HSY3RR|NPYR|CD184

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 Inhibitor:

MIP-II

Control Activator:

SDF-1a (10 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

Name

MIP-II

Measurement

11.7nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

CXCR4 antagonists may be useful for the treatment of AIDS, tumors and inflammatory diseases.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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