MLN3126

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MLN3126 (MLN 3126, MLN-3126) 是一种有效的、选择性的、口服的 CCR9 拮抗剂，IC50 为 6.3 nM（CCL25 诱导的钙动员）。

MLN3126 (MLN 3126, MLN-3126) is a potent, selective, orally available CCR9 antagonist with IC50 of 6.3 nM (CCL25-induced calcium mobilization); shows no significant antagonistic activity for other 12 chemokine receptors (CCR1, -2b, -4, -6, -7, -8, -10,CX3CR1, CXCR1, -2, -3 and -4) at 10 uM; dose dependently inhibits CCL25-induced chemotaxis of mouse thymocytes (IC90=1.8 uM); ameliorates inflammation in a T cell mediated mouse colitis model.Other Indication Phase 1 Discontinued.

MLN3126 inhibits CCL25-induced calcium mobilization with an IC50 value of 6.3 nM in CCR9 expressing cells.MLN3126 inhibits the binding of biotinylated CCL25 to CCR9 with an IC50 of 14.2 nM. Cell Invasion Assay 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.MLN3126 (0.05, 0.25 and 1% (w/w); p.o.) has the potential activity for alleviating inflammatory bowel disease (IBD). Animal Model:Activated T cell transferred colitis mouse modelDosage: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.

MLN 3126 | MLN-3126

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Other Indications

Other Disease

628300-71-0

446.902

C21H19ClN2O5S

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (55.94 mM)

——

N-{4-chloro-2-[(1-oxidopyridin-4-yl)carbonyl]phenyl}-4-(propan-2-yloxy)benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years