Niclosamide (ethanolamine salt)
(Synonyms: 氯硝柳胺乙醇胺盐,BAY2353 olamine) 目录号 : GC44400
氯硝柳胺是一种经美国食品和药物管理局 (FDA) 批准用于治疗肠道蛔虫感染的驱虫药。
Cas No.:1420-04-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Niclosamide is an anthelmintic drug approved by the US Food and Drug Administration (FDA) for treating intestinal infections of tapeworms [1,2]. The mechanism of action of the drug is to uncouple the mitochondria of the parasitic worms [1,2], and it has an excellent safety profile. Niclosamide (ethanolamine salt) is a salt form of niclosamide that has higher water solubility [1-3].
Niclosamide dose dependently inhibited STAT3-dependent luciferase reporter activity with an IC50 of 0.25 ± 0.07 μM [4]. Niclosamide inhibits Wnt/Frizzled signalling induced by the complete agonist (Wnt) with IC50 of 0.5 ± 0.05 μM [5].
Niclosamide strongly inhibited the proliferation and colony formation of Du145 prostate cancer cells with IC50 values of 0.7 and 0.1 μM. Niclosamide dose dependently induced G0/G1 phase arrest and apoptosis of Du145 cancer cells [4]. Niclosamide inhibited cell viability of 3 Adrenocortical carcinoma (ACC) cell lines BD140A, SW-13, and NCI-H295R with IC50s of 0.12 μM, 0.15 μM, and 0.53 μM, respectively [6].
Niclosamide (ethanolamine salt) (1,500 ppm in HFD(high-fat diet)) significantly reduced fasting blood glucose concentrations in mice with HFD for 4 months [3]. Niclosamide (ethanolamine salt) is rapidly metabolized by the liver, with a half-life of about 1.5 h and no accumulation in the body after several hours [3].The LD50 of Niclosamide (ethanolamine salt) in rats is 10,000 mg kg-1 body weight [3].Oral niclosamide inhibited tumor growth and the progression of human ovarian cancer and colon cancer in xenograft animal models [7,8].
References:
[1]. Frayha G J, Smyth J D, Gobert J G, et al. The mechanisms of action of antiprotozoal and anthelmintic drugs in man[J]. General Pharmacology: The Vascular System, 1997, 28(2): 273-299.
[2]. Sheth U K. Mechanisms of anthelmintic action[J]. Progress in Drug Research/Fortschritte der Arzneimittelforschung/Progrès des recherches pharmaceutiques, 1975: 147-157.
[3]. Tao H, Zhang Y, Zeng X, et al. Niclosamide ethanolamine–induced mild mitochondrial uncoupling improves diabetic symptoms in mice[J]. Nature medicine, 2014, 20(11): 1263-1269.
[4]. 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..
[5]. Chen M, Wang J, Lu J, et al. The anti-helminthic niclosamide inhibits Wnt/Frizzled1 signaling[J]. Biochemistry, 2009, 48(43): 10267-10274.
[6]. Satoh K, Zhang L, Zhang Y, et al. Identification of Niclosamide as a Novel Anticancer Agent for Adrenocortical CarcinomaNiclosamide in Adrenal Cancer[J]. Clinical Cancer Research, 2016, 22(14): 3458-3466.
[7]. King M L, Lindberg M E, Stodden G R, et al. WNT7A/β-catenin signaling induces FGF1 and influences sensitivity to niclosamide in ovarian cancer[J]. Oncogene, 2015, 34(26): 3452-3462.
[8]. Osada T, Chen M, Yang X Y, et al. Antihelminth Compound Niclosamide Downregulates Wnt Signaling and Elicits Antitumor Responses in Tumors with Activating APC MutationsNiclosamide Inhibits Wnt Signaling and Colorectal Cancer Growth[J]. Cancer research, 2011, 71(12): 4172-4182.
氯硝柳胺是一种经美国食品和药物管理局 (FDA) 批准用于治疗肠道蛔虫感染的驱虫药[1,2]。该药物的作用机制是解偶联寄生虫[1,2]的线粒体,具有极好的安全性。氯硝柳胺（乙醇胺盐）是氯硝柳胺的一种盐形式,具有较高的水溶性[1-3]。
氯硝柳胺剂量依赖性地抑制 STAT3 依赖性荧光素酶报告基因活性,IC50 为 0.25 ± 0.07 μM [4]。氯硝柳胺抑制由完全激动剂 (Wnt) 诱导的 Wnt/Frizzled 信号传导,IC50 为 0.5 ± 0.05 μM [5]。
Niclosamide 强烈抑制 Du145 前列腺癌细胞的增殖和集落形成,IC50 值为 0.7 和 0.1 μM。氯硝柳胺剂量依赖性诱导 Du145 癌细胞 G0/G1 期阻滞和凋亡[4]。氯硝柳胺抑制 3 种肾上腺皮质癌 (ACC) 细胞系 BD140A、SW-13 和 NCI-H295R 的细胞活力,IC50 分别为 0.12 μM、0.15 μM 和 0.53 μM [6]。\n
氯硝柳胺（乙醇胺盐）（在 HFD（高脂肪饮食）中为 1,500 ppm）在 4 个月内显着降低了 HFD 小鼠的空腹血糖浓度[3]。氯硝柳胺（乙醇胺盐）经肝脏快速代谢,半衰期约为1.5 h,数小时后体内无蓄积[3]。氯硝柳胺（乙醇胺盐）的LD50在体内大鼠为 10,000 mg kg-1 体重[3]。在异种移植动物模型中口服氯硝柳胺抑制肿瘤生长和人卵巢癌和结肠癌的进展[7,8].
| Cell experiment [1]: | |
|
Cell lines |
HeLa cells |
|
Preparation Method |
Cells were plated in 96-well culture plates with cell density of 3000-4000 cells/well and treated with indicated compounds by adding 100µL medium containing Niclosamide (ethanolamine salt) of various concentrations on the second day. After 72-hour's treatment, MTT was added to each well and incubated for additional 4-5 hours, and the absorbance was measured on a microplate reader at 570nm. Cell growth inhibition was evaluated as the ratio of the absorbance of the sample to that of the control. |
|
Reaction Conditions |
0.5-5µM for 72 hours |
|
Applications |
Niclosamide dose dependently inhibited STAT3-dependent luciferase reporter activity with an IC50 of 0.25 ± 0.07 µM. |
| Animal experiment [2]: | |
|
Animal models |
NOD/SCID mice |
|
Preparation Method |
HCT116 cells were harvested from flasks with 0.05% trypsin/EDTA and resuspended with Hank's buffered solution (5 × 106 cells/100 µL). CRC explants (CRC039) cultured in vitro were harvested with the same procedure and mixed with equal volume of Matrigel to make 1 × 106 cells/100 µL concentration. The cell suspensions (100 µL) were inoculated into the flanks of NOD/SCID mice. Four days later, niclosamide administration by gavage 6 d/wk for 2 (HCT116) or 3 weeks (CRC039) began. Tumor size was measured 3 times a week until mice were euthanized. |
|
Dosage form |
Niclosamide (10, 100, and 200 mg/kg) was administered by gavage for 6 d/wk for 2 (HCT116) or 3 weeks (CRC039). |
|
Applications |
In the more rapidly growing tumor (HCT116), a dose of 200 mg/kg of body weight was needed to suppress the tumor growth; 100 mg/kg of niclosamide could suppress the growth of the relatively slow-growing tumor (CRC039) to the same level. |
|
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. |
|
| Cas No. | 1420-04-8 | SDF | |
| 别名 | 氯硝柳胺乙醇胺盐,BAY2353 olamine | ||
| Canonical SMILES | OC1=C(C(NC2=CC=C([N+]([O-])=O)C=C2Cl)=O)C=C(Cl)C=C1.NCCO | ||
| 分子式 | C13H8Cl2N2O4•C2H7NO | 分子量 | 388.2 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 30 mg/mL,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/mL,Ethanol: 0.25 mg/mL | 储存条件 | Store at -20°C |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.576 mL | 12.88 mL | 25.7599 mL |
| 5 mM | 0.5152 mL | 2.576 mL | 5.152 mL |
| 10 mM | 0.2576 mL | 1.288 mL | 2.576 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet