Bindarit(Synonyms: 宾达利; AF2838)

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Bindarit (Synonyms: 宾达利; AF2838) 纯度: 99.68%

Bindarit (AF2838) 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，对其他趋化因子如 MIP-1α/CCL3，MIP-1β/CCL4，MIP-3/CCL23 无抑制作用。Bindarit 还具有抗炎作用。

Bindarit(Synonyms: 宾达利; AF2838)

Bindarit Chemical Structure

CAS No. : 130641-38-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2046 In-stock
10 mg ￥1860 In-stock
50 mg ￥5580 In-stock
100 mg ￥9300 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity[1].

IC50 & Target

MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8[1]
体外研究
(In Vitro)

Bindarit (10-300 μM; 48 hours) at 100 µM and 300 µM significantly inhibits platelet derived growth factor-BB (PDGF-BB)-induced rat VSMCs proliferation by 27% and 42%, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: VSMC cells
Concentration: 10 μM, 30 μM, 100 μM, 300 μM
Incubation Time: 48 hours
Result: Inhibited PDGF-BB-induced rat VSMCs proliferation.

体内研究
(In Vivo)

Bindarit (50 mg/kg; oral administration; every day; for 4 months, 6 months, 8 months; NZB/W F1 female mice) delays the onset of proteinuria and significantly protects from renal function impairment. Bindarit completely prevents monocyte chemoattractant protein (MCP-1) up-regulation[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NZB/W F1 female mice ( two months of age)[2]
Dosage: 50 mg/kg
Administration: Oral administration; every day; for 4 months, 6 months, 8 months
Result: Delayed the onset of proteinuria and significantly protected from renal function impairment.

Clinical Trial

分子量

324.37

Formula

C19H20N2O3
CAS 号

130641-38-2
中文名称

宾达利
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 46 mg/mL (141.81 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0829 mL 15.4145 mL 30.8290 mL
5 mM 0.6166 mL 3.0829 mL 6.1658 mL
10 mM 0.3083 mL 1.5414 mL 3.0829 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.67 mg/mL (8.23 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (8.23 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 26.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.67 mg/mL (8.23 mM); Clear solution

    此方案可获得 ≥ 2.67 mg/mL (8.23 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 26.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: 2.67 mg/mL (8.23 mM); Clear solution; Need warming

    此方案可获得 2.67 mg/mL (8.23 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 26.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Grassia, G., et al., The anti-inflammatory agent bindarit inhibits neointima formation in both rats and hyperlipidaemic mice. Cardiovasc Res, 2009. 84(3): p. 485-93.

    [2]. Zoja C, Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease. Kidney Int. 1998 Mar;53(3):726-34.

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