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Niclosamide

Niclosamide

产品编号 T0711   CAS 50-65-7
别名: BAY2353, Niclocide, 氯硝柳胺

Niclosamide (Niclocide) 是一种口服生物可利用的氯化水杨酰苯胺。它通过抑制 DNA 复制,具有驱虫和潜在的抗肿瘤活性。

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Niclosamide Chemical Structure
Niclosamide, CAS 50-65-7
规格 价格/CNY 货期 数量
500 mg ¥ 320 现货
5 g ¥ 413 现货
1 mL * 10 mM (in DMSO) ¥ 150 现货
其他形式的 Niclosamide:
产品目录号及名称: Niclosamide (T0711)
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纯度: 96.83%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Niclosamide (Niclocide)(BAY2353) is used to treat most tapeworm infections by inhibiting DNA replication.
靶点活性 STAT3:0.7 μM
体外活性 Niclosamide (< 5 μM) dose dependently inhibits STAT3-mediated luciferase reporter activity with IC50 of 0.25 μM in HeLa cells. Niclosamide(< 2 μM) dose dependently inhibits the phosphorylation of STAT3 in Du145 cells. Niclosamide (1 μM) inhibits the EGF-induced nuclear translocation of STAT3 in Du145 cells. Niclosamide(< 2 μM) dose dependently inhibits the transcription of STAT3 downstream genes in Du145 cells. Niclosamide(< 10 μM) dose dependently induces G0/G1 arrest and apoptosis of Du145 cancer cells. [1] Niclosamide is able to inhibit SARS-CoV replication at a micromolar concentration in Vero E6 cells infected with SARS-CoV. [2] Niclosamide(< 7.5 μM) promotes Frizzled1 endocytosis, downregulates Dishevelled-2 protein, and inhibits Wnt3A-stimulated beta-catenin stabilization and LEF/TCF reporter activity in U2OS cells. [3] Niclosamide inhibits the TNF-induced NF-κB reporter activity in a dose- and time-dependent manner in U2OS cells. Niclosamide(125 nM) inhibits NF-κB activation induced by p65, IKKα, IKKβ, IKKγ, and TAK1 in U2OS cells. Niclosamide(< 500 nM) completely block the time- and dose-dependent TNFα-induced alteration of the NF-κB–DNA complex in HL-60 cells. Niclosamide(< 10 nM) inhibits constitutive NF-κB activation in U266 cells. Niclosamide inhibits TNF-induced degradation of IκBα and relocation of p65 in a dose- and time-dependent manner in HL-60, Molm13, or AML primary cells. Niclosamide(500 nM) decreases TNF-induced NF-κB–dependent gene products involved in cell survival in HL-60 cells. Niclosamide dose dependently inhibits the growth and induces robust apoptosis of AML cells associated with decreased Mcl-1 and XIAP levels and increased intracellular ROS levels. [4]
体内活性 Niclosamide(40 mg/kg/d, i.p.) inhibits growth of xenografted AML cells in nude mice bearing HL-60 xenograft tumors. [4]
激酶实验 Protein Kinase profiling assay: Assay for 22 different proteins kinases is carried out by ProQinase Gmbh. All of the protein kinases are expressed either in Sf9 insect cells or in E.coli as recombinant GST-fusion proteins or His-tagged proteins. Protein kinases are purified by affinity chromatography using either GSH-agarose or Ni_NTH-agarose. A radiometric protein kinase assay is used for measuring the kinase activity of the 22 protein kinases. Briefly, for each protein kinase, 50 μL reaction cocktail containing 60 mM HEPES-NaOH, 3 mM MgCl2, 3 mM MnCl2, 3 μM Na-orthovanadate, 1.2 mM DTT, 50 μg/mL PEG20000, 1 μM [γ-33P]-ATP, Niclosamide, adequate amount of enzyme and its substrate. The PKC-alpha assay additionally contain 1 mM Cacl2, 4 mM EDTA, 5 μg/mL phosphatidylserine and 1 μg/mL 1, 2-Dioleyl-glycerol. The reaction cocktails are incubated at 37 °C for 60 minutes and stop with 50 μL 2% (v/v) H3PO4. Incorporation of 33Pi is determined with a microplate scintillation counter. The activities and the IC50 values are calculated using Quattro Workflow V2.28.
细胞实验 Cells are plated in 96-well culture plates with cell density of 3-4 &times; 103 cells/well and treat with Niclosamide by adding 100 &mu;L medium containing Niclosamide of various concentrations on the second day. After 72-hour's treatment, MTT is added to each well and incubated for additional 4-5 hours, and the absorbance is measured on a microplate reader at 570 nM. Cell growth inhibition is evaluated as the ratio of the absorbance of the sample to that of the control. The results are representative of at least 3 independent experiments. (Only for Reference)
别名 BAY2353, Niclocide, 氯硝柳胺
分子量 327.12
分子式 C13H8Cl2N2O4
CAS No. 50-65-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 6.25 mg/mL (19.11 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.057 mL 15.2849 mL 30.5698 mL 76.4246 mL
5 mM 0.6114 mL 3.057 mL 6.114 mL 15.2849 mL
10 mM 0.3057 mL 1.5285 mL 3.057 mL 7.6425 mL

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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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Ren X, et al. ACS Med Chem Lett, 2010, 1(9), 454-459. 2. Wu CJ, et al. Antimicrob Agents Chemother, 2004, 48(7), 2693-2696. 3. Chen M, et al. Biochemistry, 2009, 48(43), 10267-10274. 4. Jin Y, et al. Cancer Res, 2010, 70(6), 2516-2527.

文献引用

1. Zhao W, Xu C, Peng L, et al.cAMP/PKA signaling promotes AKT deactivation by reducing CIP2A expression, thereby facilitating decidualization.Molecular and Cellular Endocrinology.2023: 111946.
Kuraridine Milbemycin oxime Dehydrocorydaline nitrate Febantel LUPENONE Eprinomectin Oxfendazole Eugenol

相关化合物库

该产品包含在如下化合物库中:
抗癌上市药物库 抗寄生虫库 抗癌临床化合物库 抗癌活性化合物库 抗癌药物库 抗胰腺癌化合物库 抗癌化合物库 免疫/炎症分子化合物库 经典已知活性库 抗结直肠癌化合物库

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
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% Tween 80
% ddH2O
计算 重置

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

Niclosamide 50-65-7 JAK/STAT signaling Microbiology/Virology Stem Cells Antibiotic STAT Parasite BAY2353 SW-13 antihelminthic BAY-2353 inhibit BD140A Niclocide BAY 2353 NCI-H295R Vero E6 Hela Inhibitor 氯硝柳胺 bayluscide inhibitor

 

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