biological activity | ATI-2341, a peptide targeting C- X-C type 4 chemokine receptor (CXCR4), is an allosteric receptor agonist, which can activate heterotrimeric G protein (Gi), inhibit cAMP production and induce calcium mobilization. |
target | TargetValue CXCR4 (in CCRF-CEM cells) 194 nM(EC50) |
Target | Value |
CXCR4
(in CCRF-CEM cells)
| 194 nM(EC50) |
in vitro study | ATI-2341 induce CXCR4-and G protein-dependent signaling pathways, receptor in vivo migration and chemotaxis in CXCR4-expressing cells. It is an effective agonist with EC50 as 194±16 nM and intrinsic activity as 81±4%. ATI-2341 is an effective mobilizer for bone marrow polymorphonuclear neutrophils and hematopoietic stem progenitor cells, and may serve as a treatment for recruiting hematopoietic stem progenitor cells prior to autologous bone marrow transplantation. ATI-2341 can induce chemotaxis in CCRF-CEM cells. |
in vivo study | intraperitoneal injection of ATI-2341 into BALB/c mice will cause polymorphonuclear neutrophils to be recruited to the peritoneum, reaching the maximum effect when the injection concentration is 450nmol/kg. Higher concentrations will reduce the recruitment effect on cells. Intravenous injection of ATI-2341 into mice will cause a dose-dependent increase in polymorphonuclear neutrophils in the peripheral circulation. The maximum effect was achieved at an injection concentration of 0.66 μmol/kg. In the concentrations detected, ATI-2341 had no effect on lymphocyte mobilization. |