| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京