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。
| 生物活性 | 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]. |
体外研究
(In Vitro) | 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. |
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体内研究
(In Vivo) | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(55.94 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.2376 mL | 11.1882 mL | 22.3764 mL | | 5 mM | 0.4475 mL | 2.2376 mL | 4.4753 mL | | 10 mM | 0.2238 mL | 1.1188 mL | 2.2376 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
