E6130 is an orally active and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
In Vitro
E6130 is an orally active and highly selective CX3CR1 modulator, inhibits the fractalkine-induced chemotaxis of human peripheral blood natural killer cells (IC 50 , 4.9 nM), and down-regulates CX3CR1 on the cell surface of CD56 + NK cells with an EC 50 value of 5.2 nM. E6130 also shows agonistic activity via CX3CR1 with respect to GTPγS binding (EC 50 = 133 nM) and β-arrestin recruitment (EC 50 = 2.4 μM) in CX3CR1-expressing CHO-K1 membrane but show no antagonistic activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
