Catalog No.: PC-60779Not For Human Use, Lab Use Only.
E6130 is a potent, selective, orally available CX3C chemokine receptor 1 (CX3CR1) modulator that inhibits the fractalkine-induced chemotaxis of human peripheral blood NK cells with IC50 of 4.9 nM.
E6130 is a potent, selective, orally available CX3C chemokine receptor 1 (CX3CR1) modulator that inhibits the fractalkine-induced chemotaxis of human peripheral blood NK cells with IC50 of 4.9 nM.
E6130 shows no significant agonistic or antagonistic activity (EC50 and IC50>10 uM) for any other chemokine receptors.
E6130 induces the down-regulation of CX3CR1 on the cell surface of CD56+ NK cells with IC50 of 5.2 nM, shows agonistic activity with respect to [35S]GTPγS binding (EC50=133 nM) and β-arrestin recruitment (EC50=2.4 uM) in CX3CR1-expressing CHO-K1 membrane.
E6130 inhibits the migration of CX3CR1+ immune cells, and ameliorates several inflammatory bowel disease-related parameters in murine CD4+CD45RBhigh T-cell-transfer colitis model.
