E6130

E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease. IC50 & Target: CX3CR1^[1] In Vitro: E6130 is an orally active 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 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^[1]. In Vivo: E6130 (10 or 30 mg/kg, p.o.) reduces several inflammatory bowel disease-related parameters in a murine CD4⁺ CD45RB^high T-cell-transfer colitis model and a murine oxazolone-induced colitis model^[1].