Bioactivity | 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]. | |||||||||
Invitro | 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: | |||||||||
In Vivo | 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: | |||||||||
Name | CCR6 antagonist 1 | |||||||||
CAS | 588674-64-0 | |||||||||
Formula | C17H12F3NO2 | |||||||||
Molar Mass | 319.28 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [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. |