MLN3126 is an orally active and potent CCR9 antagonist. MLN3126 inhibits CCL25-induced calcium mobilization and chemotaxis of mouse primary thymocytes, wiht an IC50 value of 6.3 nM for calcium influx[1].
MLN3126 inhibits CCL25-induced calcium mobilization with an IC50 value of 6.3 nM in CCR9 expressing cells[1].
MLN3126 inhibits the binding of biotinylated CCL25 to CCR9 with an IC50 of 14.2 nM[1].
Cell Invasion Assay[1]
| Cell 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. |
MLN3126 (2.5% w/w; p.o.) decreases colonic level of IFN-γ, largely produced by T cells[1].
MLN3126 (0.05, 0.25 and 1% (w/w); p.o.) has the potential activity for alleviating inflammatory bowel disease (IBD)[1].
| Animal Model: | Activated T cell transferred colitis mouse model[1] |
| 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. |