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• 产品描述： AMG 487 是一种口服活性的、选择性的 CXC chemokine receptor 3 (CXCR3) 的拮抗剂，可抑制 IP-10 (CXCL10) 和 ITAC (CXCL11) 与 CXCR3 的结合，对应的IC50值分别为8.0 nM和8.2 nM

• 靶点： CXCR3-CXCL10(Cell-free assay):8.0 nM; CXCR3-CXCL11(Cell-free assay):8.2 nM;CXCR

• 体外研究：
  AMG487 is the targeted blocker of chemokine receptor CXCR3 and improves inflammatory symptoms by blocking the inflammatory cycle. AMG487 significantly affects DC maturity in vitro and function leading to impaired T cell activation, inducing DCs to have characteristics similar to tolerogenic DCs. AMG487 may directly play an immunomodulatory role during DC development and functional shaping

• 体内研究：
  AMG487 exhibits the antiarthritic effects in DBA/1J mice bearing collageninduced arthritis (CIA)

• 细胞实验： Cell lines: Murine bone marrow-derived DCs (BMDCs) Concentrations: 3 μM, 15 μM, 30 μM, 60 μM Incubation Time: over 6 days Method: For the analysis of the toxic effect of AMG487 on bone marrow cells and the effect of AMG487 on BMDC development, the bone marrow cells are exposed to AMG487 (3 μM, 15 μM, 30 μM, and 60 μM) from day 0, and AMG487 is supplemented with appropriate amounts every 3 days. The cells are washed twice before adding LPS to induce maturation. To investigate the effect of AMG487 on BMDC activation, we add various concentrations of AMG487 (10 μM, 30 μM, and 60 μM) only on day 6 along with the LPS. Equal amounts of the vehicle are added as a control in each case.

• 动物实验： Animal Models: DBA/1J mice Dosages: 5 mg/kg Administration: IP

• 参考文献：
  1. Michael Johnson, et al. Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. 2. Chenchen Qin, et al. In Vitro Immunological Effects of CXCR3 Inhibitor AMG487 on Dendritic Cells. Arch Immunol Ther Exp (Warsz). 2020 Apr 1;68(2):11. 3. Saleh A Bakheet, et al. CXCR3 antagonist AMG487 suppresses rheumatoid arthritis pathogenesis and progression by shifting the Th17/Treg cell balance. Cell Signal. 2019 Dec;64:109395.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.657 ml	8.284 ml	16.568 ml
  5 mM	0.331 ml	1.657 ml	3.314 ml
  10 mM	0.166 ml	0.828 ml	1.657 ml
  50 mM	0.033 ml	0.166 ml	0.331 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *