标签归档：bindarit

Bindarit(Synonyms: 宾达利; AF2838)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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  

* Please select Quantity before adding items.

Bindarit 相关产品

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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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Bindarit-d5(Synonyms: AF2838-d5)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Bindarit-d5 (Synonyms: AF2838-d5)

Bindarit-d5 (AF2838-d5) 是 Bindarit 的氘代物。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-d5(Synonyms: AF2838-d5)

Bindarit-d5 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Bindarit-d5 (AF2838-d5) is the deuterium labeled Bindarit. 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].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

329.40

Formula

C19H15D5N2O3
中文名称

宾达利 d5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. 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.

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

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Bindarit-d5(Synonyms: AF2838-d5)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Bindarit-d5 (Synonyms: AF2838-d5)

Bindarit-d5 (AF2838-d5) 是 Bindarit 的氘代物。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-d5(Synonyms: AF2838-d5)

Bindarit-d5 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Bindarit-d5 (AF2838-d5) is the deuterium labeled Bindarit. 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].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

329.40

Formula

C19H15D5N2O3
中文名称

宾达利 d5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. 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.

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

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Bindarit-d5(Synonyms: AF2838-d5)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Bindarit-d5 (Synonyms: AF2838-d5)

Bindarit-d5 (AF2838-d5) 是 Bindarit 的氘代物。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-d5(Synonyms: AF2838-d5)

Bindarit-d5 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Bindarit-d5 (AF2838-d5) is the deuterium labeled Bindarit. 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].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[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.
分子量

329.40

Formula

C19H15D5N2O3
中文名称

宾达利 d5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. 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.

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

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务