General description

A peptidomimetic derivative containing tetrahydroisoquinoline-arginine motif that aligns with a Pro-Arg motif of CXCL10. Acts as a highly specific agonist of human CXCR3 (EC₅₀ = 1.1 mM, competitive CXCL10 binding IC₅₀ = 42 nM). Does not affect murine CXCR3. Induces a long-lasting internalization of about 87% of cell-surface CXCR3 within 30 min. Effectively stimulates T-cell migration (~ 50 nM) and blocks the migration of activated T cells towards CXCL11, CXCL12, and CCL5. Also reduces the migration of activated T cells towards rheumatoid arthritis synovial fibroblasts (RASF). Shown to induce phosphorylation of ERK with similar potency and kinetics as CXCL11. Also shown to block CXCL11 induced migration of CD45+ cells to air pouches generated on humanized mice.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

O′Boyle, G., et al. 2012, PNAS.109, 4598.Stroke, I. L., et al. 2006, Biochem Biophys Res Comm.349, 221.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)