规格

价格

库存

数量

500 mg

¥ 320

现货

5 g

¥ 413

现货

1 mL x 10 mM (in DMSO)

¥ 150

现货

生物活性

产品描述	Niclosamide is a classic salicylanilide antiparasitic drug and a multi-target, low-toxicity, broad-spectrum small-molecule modulator with anthelmintic and antitumor activity. Niclosamide disrupts the parasite’s energy metabolism by uncoupling mitochondrial oxidative phosphorylation, leading to reduced ATP production and ultimately killing the parasite. Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells.
靶点活性	STAT3:0.7 μM
体外活性	方法：从 MDA-MB-231 细胞中分离的 CD44⁺/CD24⁻ 乳腺癌干细胞（CSCs）加入 Niclosamide （100 μM），处理 6 小时，Western blot 检测 p-STAT3， STAT3， Bax 蛋白水平。结果：Niclosamide 诱导 p-STAT3 水平显著降低，促凋亡蛋白 Bax 水平显著升高。[1]
体内活性	方法：13 周龄雄性 SOD1-G93A 小鼠腹腔注射 Niclosamide (20 mg/kg 或 50 mg/kg)，每日一次，直至终末期(约 160 天)。结果：20 mg/kg Niclosamide 效果显著，改善神经学评分，延缓运动功能衰退，显著延长生存期，提高疾病各阶段的生存概率。[2] 方法：雄性 db/db 小鼠(2 型糖尿病模型)，所有小鼠在 8 周龄时行右侧肾切除术以加速 DN 发展，手术后腹腔注射 Niclosamide (20 mg/kg/天)，每日一次，连续 4 周。结果：Niclosamide 显著降低血糖和 HbA1c，减少尿量，改善 BUN 和 Cr，并阻止了尿白蛋白的进行性增加，减轻肾脏肥大、肾小球硬化、系膜扩张和 Col-IV 沉积；恢复 nephrin 表达和足细胞数量。[3]
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 × 103 cells/well and treat with Niclosamide by adding 100 μL 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	氯硝柳胺, Niclocide, BAY2353

化学信息

分子量	327.12
分子式	C₁₃H₈Cl₂N₂O₄
CAS No.	50-65-7
Smiles	C(NC1=C(Cl)C=C(N(=O)=O)C=C1)(=O)C2=C(O)C=CC(Cl)=C2
密度	1.6646 g/cm3 (Estimated)

储存&溶解度

存储

Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

DMSO: 6.25 mg/mL (19.11 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 0.63 mg/mL (1.93 mM), Solution.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0570 mL	15.2849 mL	30.5698 mL	152.8491 mL
5 mM	0.6114 mL	3.0570 mL	6.1140 mL	30.5698 mL
10 mM	0.3057 mL	1.5285 mL	3.0570 mL	15.2849 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

Niclosamide

Niclosamide

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Niclosamide

Niclosamide

Niclosamide 相关产品

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