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Bindarit

现货
Catalog No.
B2156
CCL2, CCL7,CCL8 抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,540.00
现货
5mg
¥ 1,190.00
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25mg
¥ 3,290.00
现货
50mg
¥ 4,690.00
现货
200mg
¥ 11,690.00
现货

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Background

Bindarit(AF-2838), an anti-inflammatory agent, is a selective inhibitor againstmonocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8[1].

MCP-1, MCP-2, and MCP-3 are inflammatory mediators that specifically stimulate the directional migration of T cells as well as monocytes and may play an important role in immune cell recruitment into sites of antigenic challenge [2].

In vitro: Bindarit inhibited MCP-1 and TNF-alpha production induced in monocytes by LPS and Candida albicans in a dose-dependent manner with the IC50 of 172 µM and 403 µM, respectively.The inhibition of LP-induced MCP-1 production by Bindarit has been associated with the reduced levels of MCP-1 mRNA transcripts with the IC50 value of 75 µM. Bindaritexihibited an inhibitory effect in the production of MCP-1 by LPS-stimulated MM6 cells with an IC50 of 425 μM, without affecting the release of IL-8 or IL-6[3].Administration of bindarit (10-300 μM) reduced rat vascular smooth muscle cell (VSMC) proliferation, migration, and invasion[4].

In vivo: In NZB/W mice model with lupus nephritis, oral treatment of bindarit prolonged survival and delayed the onset of proteinuria [3]. In rats treated with bindarit (200 mg/kg/day), bindarit resulted in a 39% reduction of balloon injury-induced neointima formation at day 14 without affecting re-endothelialization. Bindarit reduced the number of medial and neointimal proliferating cells at day 7 by 54 and 30%, respectively. In hypercholesterolaemicapoE(-/-) mice, administration of bindarit reduced the number of proliferating cells by 42%at day 7 after carotid injury and inhibited of neointima formation by 47% at day 28. In neointimal lesions of apoE(-/-) mice treated with bindarit, data analysis of the cellular composition showed that the relative content of macrophages and the number of VSMCs were reduced by 66 and 30%, respectively, compared with the control group[4].

References:
[1]. Zoja C, Corna D, Benedetti G, et al. Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease[J]. Kidney international, 1998, 53(3): 726-734.
[2]. Taub D D, Proost P, Murphy W J, et al. Monocyte chemotactic protein-1 (MCP-1),-2, and-3 are chemotactic for human T lymphocytes[J]. Journal of Clinical Investigation, 1995, 95(3): 1370.
[3]. Sironi M, Guglielmotti A, Polentarutti N, et al. A small synthetic molecule capable of preferentially inhibiting the production of the CC chemokine monocyte chemotactic protein-1[J]. European cytokine network, 1999, 10(3): 437-442.
[4]. Grassia G, Maddaluno M, Guglielmotti A, et al. The anti-inflammatory agent bindarit inhibits neointima formation in both rats and hyperlipidaemicmice[J]. Cardiovascular research, 2009, 84(3): 485-493.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt324.37
Cas No.130641-38-2
FormulaC19H20N2O3
Solubility≥16.2mg/mL in DMSO
Chemical Name2-[(1-benzylindazol-3-yl)methoxy]-2-methylpropanoic acid
SDFDownload SDF
Canonical SMILESCC(C)(C(=O)O)OCC1=NN(C2=CC=CC=C21)CC3=CC=CC=C3
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

大鼠血管平滑肌细胞 (VSMCs)

制备方法

在DMSO中的溶解度大于16.2 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

10 ~ 300 μM

实验结果

在100 μM和300 μM剂量下,Bindarit显著抑制PDGF-BB诱导的大鼠VSMC增殖(分别为27%和42%)。此外,在PDGF-BB刺激的VSMCs中,Bindarit (10 ~ 300 μM) 呈浓度依赖性地抑制MCP-1产生。

动物实验 [1]:

动物模型

ApoE-/-小鼠

给药剂量

100 mg/kg;口服给药;每天2次

实验结果

在ApoE-/-小鼠中,Bindarit显著减少PCNA阳性细胞数量以及新生内膜面积。在新生内膜损伤部位,Bindarit还降低F4/80阳性巨噬细胞的相对含量 (66%) 以及VSMC的数量 (30%)。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Grassia G, Maddaluno M, Guglielmotti A, et al. The anti-inflammatory agent bindarit inhibits neointima formation in both rats and hyperlipidaemicmice[J]. Cardiovascular research, 2009, 84(3): 485-493.

质量控制

化学结构

Bindarit