E6130 may be effective in the treatment of inflammatory bowel disease and is a highly selective CX3CR1 regulator for oral administration.

E6130 also shows agonistic activity via CX3CR1 with respect to GTPγS binding (EC50 = 133 nM) and β-arrestin recruitment (EC50 = 2.4 μM) in CX3CR1-expressing CHO-K1 membrane but show no antagonistic activity.E6130 is an orally available and highly selective CX3CR1 modulator, inhibits the fractalkine-induced chemotaxis of human peripheral blood natural killer cells (IC50, 4.9 nM), and down-regulates CX3CR1 on the cell surface of CD56+ NK cells with an EC50 value of 5.2 nM.

E6130(10 or 30mg /kg, p.o.) reduced some parameters associated with inflammatory bowel disease in a mouse model of CD4+ CD45RBhigh t cell metastatic colitis and a mouse model of oxazolidin-induced colitis.

1427058-33-0

C28H37ClF3N3O3

556.06

DMSO:250 mg/mL (449.59 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years