Niclosamide
(Synonyms: 氯硝柳胺; BAY2353) 目录号 : GC13586
Niclosamide是一种驱虫药，是STAT3的小分子抑制剂，IC50值为0.25±0.07μM。
Cas No.:50-65-7
Sample solution is provided at 25 µL, 10mM.
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Niclosamide, an anthelmintic drug, is the small-molecule inhibitor of STAT3 with an IC50 value of 0.25±0.07μM[1]. Niclosamide has been widely used in cancer research and metabolic regulation studies, and is employed as a model compound to develop a series of derivatives[2].
In vitro, Niclosamide treatment for 3 days significantly inhibited the viability of HL-60 cells, with an IC50 value of 0.28 ± 0.03μM[3]. Treatment with 0.6µM Niclosamide for 24 hours significantly inhibited the expression of LRP6 in HEK293 cells and blocked the activation of the Wnt/β-catenin signaling pathway[4]. Treatment with 20μM Niclosamide for 24 hours significantly inhibited the viability of TPC-1 cells, causing the cells to become vacuolated and disintegrated[5]. Treatment with 0.5μM Niclosamide for 12 hours significantly inhibited the migration rate of BD140A cells and reduced the levels of epithelial-mesenchymal transition mediators (N-cadherin and vimentin)[6].
In vivo, Niclosamide treatment via daily intraperitoneal injection at a dose of 10mg/kg for 21 days can significantly alleviate the pulmonary fibrosis symptoms induced by bleomycin in mice and inhibit the accumulation of collagen[7]. Oral administration of Niclosamide at a dose of 200mg/kg/day for 9 weeks improved myocardial hypertrophy, cardiac fibrosis and cardiac dysfunction in mice with aortic coarctation [8].
References:
[1] Ren X, Duan L, He Q, et al. Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway[J]. ACS medicinal chemistry letters, 2010, 1(9): 454-459.
[2] Kang B, Mottamal M, Zhong Q, et al. Design, synthesis, and evaluation of niclosamide analogs as therapeutic agents for enzalutamide-resistant prostate cancer[J]. Pharmaceuticals, 2023, 16(5): 735.
[3] Chae H D, Cox N, Dahl G V, et al. Niclosamide suppresses acute myeloid leukemia cell proliferation through inhibition of CREB-dependent signaling pathways[J]. Oncotarget, 2017, 9(4): 4301.
[4] Lu W, Lin C, Roberts M J, et al. Niclosamide suppresses cancer cell growth by inducing Wnt co-receptor LRP6 degradation and inhibiting the Wnt/β-catenin pathway[J]. PloS one, 2011, 6(12): e29290.
[5] Yu K, Wang T, Li Y, et al. Niclosamide induces apoptosis through mitochondrial intrinsic pathway and inhibits migration and invasion in human thyroid cancer in vitro[J]. Biomedicine & Pharmacotherapy, 2017, 92: 403-411.
[6] Satoh K, Zhang L, Zhang Y, et al. Identification of niclosamide as a novel anticancer agent for adrenocortical carcinoma[J]. Clinical Cancer Research, 2016, 22(14): 3458-3466.
[7] Boyapally R, Pulivendala G, Bale S, et al. Niclosamide alleviates pulmonary fibrosis in vitro and in vivo by attenuation of epithelial-to-mesenchymal transition, matrix proteins & Wnt/β-catenin signaling: A drug repurposing study[J]. Life sciences, 2019, 220: 8-20.
[8] Fu Y, Hu N, Cao M, et al. Anthelmintic niclosamide attenuates pressure-overload induced heart failure in mice[J]. European Journal of Pharmacology, 2021, 912: 174614.
Niclosamide是一种驱虫药，是STAT3的小分子抑制剂，IC50值为0.25±0.07μM[1]。该药物广泛应用于癌症研究和代谢调控研究，并作为先导化合物用于开发系列衍生物[2]。
在体外，Niclosamide处理3天可显著抑制HL-60细胞活力，IC50值为0.28±0.03μM[3]。0.6µM的Niclosamide处理HEK293细胞24小时能显著抑制LRP6表达并阻断Wnt/β-catenin信号通路激活[4]。20μM的Niclosamide处理TPC-1细胞24小时可显著抑制细胞活力，导致细胞空泡化并解体[5]。0.5μM的Niclosamide处理BD140A细胞12小时能显著抑制细胞迁移率，降低上皮-间质转化介质（N-钙黏蛋白和波形蛋白）水平[6]。
在体内，小鼠每日腹腔注射Niclosamide（10mg/kg；持续21天）可显著缓解博来霉素诱导的肺纤维化症状并抑制胶原沉积[7]。主动脉缩窄小鼠每日口服200mg/kg剂量的Niclosamide（持续9周）能改善心肌肥大、心脏纤维化和心功能障碍[8]。
| Cell experiment [1]: | |
Cell lines | TPC-1 cells |
Preparation Method | The TPC-1 cells were cultured in RPIM 1640 medium containing 10% heat-inactivated fetal bovine serum (FBS) and 1% antibiotics (penicillin and streptomycin) at 37°C and 5% CO2. The exponentially growing TPC-1 cells (3000-5000 cells per well) were seeded in 96-well plates. After incubation for 24 hours, the cells were treated with different concentrations of Niclosamide (0, 1.25, 2.5, 5, 10, and 20μM). Each treatment was carried out for 24 hours, and 20μL of 5mg/mL MTT was added to each well and incubated at 37°C. The medium was removed, and 150μL DMSO was added to each well to dissolve the methylene blue. The absorbance was recorded at 570nm. |
Reaction Conditions | 0, 1.25, 2.5, 5, 10, and 20μM; 24h |
Applications | Niclosamide treatment significantly inhibited the viability of TPC-1 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Swiss albino mice |
Preparation Method | Eight-week-old male Swiss albino mice were raised in a standard environment with free access to food and water, and were maintained under a 12/12 light-dark cycle. The mice were randomly divided into the following groups (n=10): control group; Bleomycin alone group (1.5IU/kg Bleomycin); Bleomycin + Niclosamide group (10mg/kg). DMSO and polyethylene glycol 200 (in a ratio of 1:4) were used as the carrier for Niclosamide administration in the physiological saline. The DMSO concentration was 1% in the saline. The required amount of Niclosamide was weighed, dissolved in DMSO:PEG (1:4 ratio) saline, and the probes were thoroughly treated with ultrasound before administration. Mice were injected with 1.5IU/kg Bleomycin on the 0th day, and intraperitoneally injected Niclosamide once daily from the 1st to the 21st day. On the day of the end of the experiment (the 21st day), lung tissues were taken and preserved for evaluating various biochemical parameters, pathology and molecular biology studies. |
Dosage form | 10mg/kg for 21 days; i.p. |
Applications | Niclosamide treatment alleviated pulmonary fibrosis induced by bleomycin in mice. |
References: | |
| Cas No. | 50-65-7 | SDF | |
| 别名 | 氯硝柳胺; BAY2353 | ||
| 化学名 | 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide | ||
| Canonical SMILES | C1=CC(=C(C=C1[N+](=O)[O-])Cl)NC(=O)C2=C(C=CC(=C2)Cl)O | ||
| 分子式 | C13H8Cl2N2O4 | 分子量 | 327.12 |
| 溶解度 | ≥ 12.75mg/mL in EtOH with gentle warming; 4.55 mg/mL in DMSO (Need ultrasonic) | 储存条件 | Store at RT |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.057 mL | 15.2849 mL | 30.5698 mL |
| 5 mM | 0.6114 mL | 3.057 mL | 6.114 mL |
| 10 mM | 0.3057 mL | 1.5285 mL | 3.057 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.50%
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