貨號	規格	價格	上海	北京	武漢	南京
S85480-5mg	99.4%	￥680.00 S85480-5mg ￥680.00 現貨	3 3	-	-	-
S85480-10mg	99.4%	￥1030.00 S85480-10mg ￥1030.00 現貨	4 4	-	-	-
S85480-25mg	99.4%	￥2040.00 S85480-25mg ￥2040.00 現貨	5 5	-	-	-
S85480-100mg	≥98%	￥5900.00 S85480-100mg ￥5900.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

AMG 487 是一種口服活性的、選擇性的 CXC chemokine receptor 3 (CXCR3) 的拮抗劑，可抑制 IP-10 (CXCL10) 和 ITAC (CXCL11) 與 CXCR3 的結合，對應的IC50值分別為8.0 nM和8.2 nM

產品描述：

AMG 487 是一種口服活性的、選擇性的 CXC chemokine receptor 3 (CXCR3) 的拮抗劑，可抑制 IP-10 (CXCL10) 和 ITAC (CXCL11) 與 CXCR3 的結合，對應的IC50值分別為8.0 nM和8.2 nM

靶點：

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

體外研究：

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

體內研究：

AMG487 exhibits the antiarthritic effects in DBA/1J mice bearing collageninduced arthritis (CIA)

細胞實驗：

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.

動物實驗：

Animal Models: DBA/1J mice Dosages: 5 mg/kg Administration: IP

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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