CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs)[1].
CCR6 antagonist 1 (compound 1b, 50 μM, 3 h) blocks the CCL20-induced CD4+ T cell migration[1].
CCR6 antagonist 1 (30 nM-300 μM, 20 min) inhibits miniGi recruitment to CCR6 induced by CCL20, and β-arrestin-1 recruitment to CCR6 and CCR5 by CCL20 and CCL5 (5 nM), respectively[1].
Cell Migration Assay [1]
| Cell Line: | CCL20 (500 ng/mL)-induced CCR6+CD4+ T cell |
| Concentration: | 0.5, 5, 50 μM |
| Incubation Time: | 3 h |
| Result: | Inhibited CCL20-induced cell migration at 50 μM. |
CCR6 antagonist 1 (compound 1b, 1 mg/kg, s.c., twice daily for 3 days) alleviates TNBS-induced inflammatory responses in mice[1].
CCR6 antagonist 1 (1 mg/kg, s.c., twice, before and after zymosan treatment) shows anti-inflammatory effects
in Zymosan-induced peritonitis mice[1].
| Animal Model: | Murine model of colitis (5 mg/mouse TNBS-induced)[1] |
| Dosage: | 1 mg/kg |
| Administration: | Subcutaneous injection (s.c.), twice daily for 3 days. |
| Result: | Improved mice general conditions, attenuated macroscopic injury and counteracted neutrophils infiltration, both in the colon and in lungs. |
| Animal Model: | Zymosan-induced peritonitis mice[1] |
| Dosage: | 1 mg/kg |
| Administration: | Subcutaneous injection (s.c.), twice, before and after zymosan treatment |
| Result: | Significantly reduced the total protein content and myeloperoxidase activity in the peritoneal lavage. |
[1]. Maria Grazia Martina, et al. Discovery of small-molecules targeting the CCL20/CCR6 axis as first-in-class inhibitors for inflammatory bowel diseases. Eur J Med Chem. 2022 Aug 29;243:114703.