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Bindarit

Bindarit

产品编号 T6413   CAS 130641-38-2
别名: 宾达利, AF2838

Bindarit 是单核细胞趋化蛋白MCP-1/CCL2,MCP-3/CCL7和MCP-2/CCL8的选择性抑制剂,具有抗炎作用。

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Bindarit, CAS 130641-38-2
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产品目录号及名称: Bindarit (T6413)
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纯度: 98.71%
纯度: 98.48%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Bindarit displays specific inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.
体外活性 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. [2] Bindarit treatment inhibits the release of MCP-1 from IL-1 stimulated osteoblast cell line Saos-2. [3] 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. [4] Bindarit (10-300 μM) reduces rat vascular smooth muscle cell (VSMC) proliferation, migration, and invasion. [5] 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. [6] Bindarit modulates cancer-cell proliferation and migration, mainly through negative regulation of TGF-β and AKT signaling. [7]
体内活性 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. [1] Inhibition of MCP-1 with Bindarit also reduces tumor growth and macrophage recruitment, rendering necrotic tumor masses in human melanoma xenografts. [4] 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. [5] 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. [7]
别名 宾达利, AF2838
分子量 324.37
分子式 C19H20N2O3
CAS No. 130641-38-2

存储

 | Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

Ethanol: 25 mg/mL(77.1 mM)

DMSO: 65 mg/mL (200.38 mM)

H2O: <1 mg/mL

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Zoja C, et al. Kidney Int, 1998, 53(3), 726-734. 2. Sironi M, et al. Eur Cytokine Netw, 1999, 10(3), 437-442. 3. Guglielmotti A, et al. Inflamm Res, 2002, 51(5), 252-258. 4. Gazzaniga S, et al. J Invest Dermatol, 2007, 127(8), 2031-2041. 5. Grassia G, et al. Cardiovasc Res, 2009, 84(3), 485-493. 6. Wu R, Zhang P A, Liu X, et al. Decreased miR-325-5p Contributes to Visceral Hypersensitivity Through Post-transcriptional Upregulation of CCL2 in Rat Dorsal Root Ganglia[J]. Neuroscience bulletin. 2019 Apr 12: 1-11.

文献引用

1. Wu R, Zhang P A, Liu X, et al. Decreased miR-325-5p Contributes to Visceral Hypersensitivity Through Post-transcriptional Upregulation of CCL2 in Rat Dorsal Root Ganglia. Neuroscience Bulletin. 2019 Apr 12: 1-11 2. Shi Z, Yu P, Lin W J, et al.Microglia drive transient insult-induced brain injury by chemotactic recruitment of CD8+ T lymphocytes.Neuron.2023
MLN-3897 CCR3 antagonist 1 BMS-817399 CCR2 antagonist 5 CCR1 antagonist 6 CCX354 PF-04634817 Cenicriviroc Mesylate

相关化合物库

该产品包含在如下化合物库中:
经典已知活性库 已知活性化合物库 临床期小分子药物库 肿瘤免疫治疗小分子化合物库 抗代谢疾病化合物库 天然产物库 抗感染天然产物库 抗COVID-19化合物库 抗糖尿病库 抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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X
X
X
=
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g/mol

输入分子式,点击计算,可计算出产品的分子量。

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Bindarit 130641-38-2 Immunology/Inflammation Microbiology/Virology CCR 宾达利 AF 2838 AF2838 inhibit CC chemokine receptor Inhibitor AF-2838 inhibitor

 

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