MLN3126

MLN3126 is an orally active and potent CCR9 antagonist. MLN3126 inhibits CCL25-induced calcium mobilization and chemotaxis of mouse primary thymocytes, wiht an IC 50 value of 6.3 nM for calcium influx. In Vitro MLN3126 inhibits CCL25-induced calcium mobilization with an IC 50 value of 6.3 nM in CCR9 expressing cells. MLN3126 inhibits the binding of biotinylated CCL25 to CCR9 with an IC 50 of 14.2 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Invasion AssayCell Line: Mouse thymocytes Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 μM Incubation Time: 90 min Result: Inhibited CCL25-induced chemotaxis of mouse thymocytes. In Vivo MLN3126 (2.5% w/w; p.o.) decreases colonic level of IFN-γ, largely produced by T cells . MLN3126 (0.05, 0.25 and 1% (w/w); p.o.) has the potential activity for alleviating inflammatory bowel disease (IBD) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Activated T cell transferred colitis mouse model Dosage: 0.05, 0.25 and 1% (w/w) (around 4 g/day) Administration: Oral gavage; 21 days Result: Blocked CCR9/CCL25 interaction by inhibiting migration of T cells to the colon and resulted in the amelioration of colitis. Form:Solid

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