MLN3126 是一种具有口服活性的强效 CCR9 拮抗剂。 MLN3126 抑制 CCL25 诱导的钙动员 (calcium mobilization) 和小鼠初级胸腺细胞趋化 (chemotaxis)，抑制钙内流的 IC50 为 6.3 nM。
| Cas No. | 628300-71-0 |
| 分子式 | C21H19ClN2O5S |
| 分子量 | 446.9 |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | MLN3126 is an orally active and potentCCR9antagonist. MLN3126 inhibits CCL25-induced calcium mobilization and chemotaxis of mouse primary thymocytes, wiht anIC50value of 6.3 nM forcalcium influx[1]. MLN3126 inhibits CCL25-induced calcium mobilization with an IC50value of 6.3 nM in CCR9 expressing cells[1].
MLN3126 inhibits the binding of biotinylated CCL25 to CCR9 with an IC50of 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. |
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