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CCR6 antagonist 1

目录号 : GC67788

CCR6 antagonist 1 是一种 CCR6 拮抗剂,可抑制 CCL20/CCR6 信号通路。 CCR6 antagonist 1 可用于自身免疫介导的炎症性疾病的研究,如炎症性肠病 (IBDs)。

CCR6 antagonist 1 Chemical Structure

Cas No.:588674-64-0

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10 mM * 1mLinDMSO
¥713.00
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5mg
¥648.00
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10mg
¥1,008.00
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25mg
¥2,088.00
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50mg
¥3,024.00
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100mg
¥4,680.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 588674-64-0 SDF Download SDF
分子式 C17H12F3NO2 分子量 319.28
溶解度 DMSO : ≥ 100 mg/mL (313.20 mM) 储存条件 Store at -20°C
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1 mM 3.132 mL 15.6602 mL 31.3205 mL
5 mM 0.6264 mL 3.132 mL 6.2641 mL
10 mM 0.3132 mL 1.566 mL 3.132 mL
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