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  • Bindarit
    • 宾达利;AF2838;AF-2838;AF 2838
    货号: abs810272
    CAS号: 130641-38-2
    分子式: C19H20N2O3
    分子量: 324.37
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810272-5mg 1-2周 ¥1313.00
    - +
    abs810272-10mg 1-2周 ¥1806.00
    - +
    abs810272-50mg 1-2周 ¥5408.00
    - +
    abs810272-100mg 1-2周 ¥9030.00
    - +
    大包装询价
    产品描述
    描述
    Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.
    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    宾达利;AF2838;AF-2838;AF 2838
    外观
    White to off white Powder
    可溶性/溶解性
    DMSO :65 mg/mL (200.38 mM)
    Ethanol :65 mg/mL (200.38 mM)
    生物活性
    靶点
    MCP-1/CCL2;MCP-3/CCL7;MCP-2/CCL8
    In vitro(体外研究)
    Bindarit treatment causes a dose-dependent inhibition of the capacity of human monocytes to produce monocyte chemotactic protein-1 (MCP-1) in response to bacterial LPS or C. albicans with IC50 of 172 µM and 403 µM, respectively. The inhibition of LP-induced MCP-1 production by Bindarit is associated with reduced levels of MCP-1 mRNA transcripts with IC50 of 75 µM. Bindarit inhibits the production of MCP-1 by LPS-stimulated MM6 cells with IC50 of 425 μM, without affecting the release of IL-8 or IL-6. Bindarit treatment inhibits the release of MCP-1 from IL-1 stimulated osteoblast cell line Saos-2. Bindarit, even at the maximal concentration, does not exhibit a direct in vitro cytotoxic effect on human IIB-MEL-J melanoma or ECs, although it inhibits MCP-1 expression. Bindarit (10-300 μM) reduces rat vascular smooth muscle cell (VSMC) proliferation, migration, and invasion. Bindarit induces the downregulation of the classical NF-κB pathway. Bindarit displays a specific inhibitory effect on the p65 and p65/p50 induced MCP-1 promoter activation, with no effect on other tested activated promoters, indicating that Bindarit acts on a specific subpopulation of NF-κB isoforms and selects its targets within the whole NF-κB inflammatory pathway. Bindarit modulates cancer-cell proliferation and migration, mainly through negative regulation of TGF-β and AKT signaling.
    In vivo(体内研究)
    Oral administration of Bindarit at 50 mg/kg in NZB/W mice delays the onset of proteinuria, significantly protects from renal function impairment, and prolongs survival of NZB/W mice or lupus mice. Bindarit treatment completely MCP-1 up-regulation during the progression of nephritis. Inhibition of MCP-1 with Bindarit also reduces tumor growth and macrophage recruitment, rendering necrotic tumor masses in human melanoma xenografts. Bindarit is effective in reducing neointima formation in both non-hyperlipidaemic and hyperlipidaemic animal models of vascular injury by a direct effect on VSMC proliferation and migration and by reducing neointimal macrophage content. Administration of Bindarit results in impaired metastatic disease in prostate cancer PC-3M-Luc2 xenograft mice and impairment of local tumorigenesis in Balb/c mice with murine breast cancer 4T1-Luc cells. In addition, Bindarit treatment significantly decreases the infiltration of tumor-associated macrophages and myeloid-derived suppressor cells in 4T1-Luc primary tumors.
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
    • 实验方法 实验条件
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