计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
Information
Bindarit (AF 2838) Bindarit (AF 2838) exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.
In vitro
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
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.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
别名
宾达里特 (AF 2838)
英文别名
2-((1-benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Bindarit (AF 2838)
生化机理
Bindarit (AF 2838) 对单核细胞趋化蛋白 MCP-1/CCL2、MCP-3/CCL7 和 MCP-2/CCL8 具有选择性抑制作用。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
脂肪酸结合蛋白 4 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)(C(=O)O)OCC1=NN(C2=CC=CC=C21)CC3=CC=CC=C3
分子量
324.37
Reaxy-Rn
14755397
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14755397&ln=
技术文档
高级数据
关联靶点（人）
FABP4
Tchem
脂肪酸结合蛋白、脂肪细胞(Fatty acid-binding protein, adipocyte)
(0 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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