CXCR3 Agonist, PS372424

CXCR3 Agonist, PS372424
(S)-N-((S)-1-((cyclohexylmethyl)amino)-5-guanidino-1-oxopentan-2-yl)-2-(4-oxo-4-phenylbutanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, Chemokine (C-X-C motif) Receptor 3 Agonist
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.
产品信息
Form  White powder
Formulation  Supplied as a trifluoroacetate salt.
Molar mass  588.7
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥97% by HPLC
Solubility  DMSO
Chemical formula  C33H44N6O4 • 3H2O
商店和运输信息
Storage  +2°C to +8°C
Ship  Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling