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编 号:F740945
分子式:C17H12F3NO2
分子量:319.28
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
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).

体内研究:
CCR6 拮抗剂 1 (化合物 1b,1 mg/kg,皮下注射,每天两次,持续 3 天) 减轻 TNBS 诱导的小鼠炎症反应。 CCR6 拮抗剂 1 (1 mg/kg,sc,twice,before和after zymosan treatment) 在酵母聚糖诱导的腹膜炎小鼠中表现出抗炎作用。Animal Model:Murine model of colitis (5 mg/mouse TNBS-induced)
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
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.

体外研究:
CCR6 antagonist 1 (化合物 1b,50 μM,3 小时) 阻断 CCL20 诱导的 CD4+ T 细胞迁移。 CCR6 antagonist 1 (30 nM-300 μM,20 分钟) 分别抑制 CCL20 诱导的 miniGi 募集到 CCR6,以及 CCL20 和 CCL5 (5 nM) 诱导的 β-arrestin-1 募集到 CCR6 和 CCR5。
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