Niclosamide|50-65-7|(氯硝柳胺; BAY2353)-陌孚医药/Medlife

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Niclosamide (Synonyms: 氯硝柳胺; BAY2353)

目录号: PC11654 纯度: ≥98%

CAS No. :50-65-7

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中文名称

Niclosamide

中文别名

氯硝柳胺;N-(2'-氯-4'-硝基苯)-5-氯水杨酰胺;2',5-二氯-4'-硝基水杨酸酰替苯胺;4'-硝基-2',5-二氯水杨酰苯胺;杀螺胺;贝螺杀;百螺杀;氯螺消;lu硝柳胺;甲磺酸多沙唑嗪;氯硝柳胺 EP标准品;氯硝柳胺标准品;氯硝柳胺-13C6;氯硝柳胺-D6;清塘净;无水氯硝柳胺;2,5-二氯-4-硝基水杨酸酰替苯胺;4-硝基-2,5-二氯水杨酰苯胺;5,2'-二氯-4'-硝基水杨酰替苯胺;见螺杀;氯硝柳胺,灭绦灵;灭绦录;耐克螺;杀鳗剂;血防-67;育末生;2′,5-二氯-4′-硝基水杨酸酰替苯胺;氯硝柳胺原料药生产厂家;表面接触皿TSA

英文名称

Niclosamide

英文别名

niclosamide;2,5-dichloro-4-nitrosalicylanilide;6-Benzylamino-2(R)-[[1-(hydroxymethyl)-propyl]amino-9-isopropylpurin];bayluscid;2',5-dichloro-4'-nitrosalicylanilide;2-hydroxy-5-chloro-n-(2-chloro-4-nitrophenyl)benzamide;5-chloro-2'-chloro-4'-nitrosalicylanilide;5-chloro-n-(2-chloro-4-nitrophenyl)salicylamide;Bayer 25648,Bayluscide;Bayer 73;Clonitralid;SR 73;BAY2353;Niclosamide (Niclocide®);2’,5-dichloro-4’-nitrosalicylanilide;5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxybenzamide;5-CHLORO-N-(2-CHLORO-4-NITROPHENYL)-SALICYLAMIDE;b2353;fenasal;hl2447;iomesan;iomezan;lintex;mato;nasemo;sulqui;Niclocide;Tredemine;Phenasal;Yomesan;Helmiantin;Dichlosale;Atenase;Devermin;Cestocid;Vermitid;Radeverm;Mansonil;Sagimid;Devermine;Fedal-Telmin;Zestocarp;Radewerm;Bayer 2353;Chemagro 2353;Benzamide, 5-chloro-N-(2-chloro-4-nitrophenyl)-2-hydroxy-;BAY 2353;nicolsamide;HL 2447;Nic

Cas No.

50-65-7

分子式

C₁₃H₈Cl₂N₂O₄

分子量

327.12

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research. Niclosamide is a STAT3 inhibitor with an IC₅₀ of 0.25 μM in HeLa cells. Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells.

性状

Solid

IC50 & Target[1][2]

STAT3

0.25 μM (IC₅₀, in HeLa cells)

体外研究(In Vitro)

Niclosamide (0.6 nM-46 μM) treatment inhibits adrenocortical carcinoma cellular proliferation in BD140A, SW-13, and NCI-H295R cells.
Niclosamide (0.05-5 μM, 24 h) treatment inhibits STAT3-mediated luciferase reporter activity in HeLa cells .
Niclosamide (10 μM) treatment inhibits virus replication in Vero E6 cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	BD140A, SW-13 and NCI-H295R cells
Concentration:	0.6 nM-46 μM
Incubation Time:
Result:	Inhibited cellular proliferation in adrenocortical carcinoma cell lines with the IC₅₀ of 0.12 μM, 0.15 μM, and 0.53 μM in BD140A, SW-13, and NCI-H295R, respectively.

Cell Viability Assay

Cell Line:	Hela cells
Concentration:	0.05-5 μM
Incubation Time:	24 hours
Result:	Inhibited STAT3-mediated luciferase reporter activity with an IC₅₀ of 0.25 μM.

Cell Viability Assay

Cell Line:	Vero E6 cells
Concentration:	10 μM
Incubation Time:	2 days
Result:	Inhibited the synthesis of viral antigens of SARS-CoV in Vero E6 cells.

体内研究(In Vivo)

Niclosamide (oral gavage; 100 mg/kg, 200 mg/kg; once a week; 8 weeks) treatment inhibits adrenocortical carcinoma tumor growth in vivo.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nu/Nu mice injected with NCI-H295R cells
Dosage:	100 mg/kg, 200 mg/kg
Administration:	Oral gavage; 100 mg/kg, 200 mg/kg; once a week; 8 weeks
Result:	Showed a 60%-80% inhibition in tumor growth, as compared to the control group.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. P Andrews, et al. The biology and toxicology of molluscicides, Bayluscide. Pharmacol Ther. 1982;19(2):245-95. [Information]

[2]. Wei Chen, et al. Niclosamide: Beyond an antihelminthic drug. Cell Signal. 2018 Jan;41:89-96. [Information]

[3]. Kei Satoh, et al. Identification of Niclosamide as a Novel Anticancer Agent for Adrenocortical Carcinoma. Clin Cancer Res. 2016 Jul 15;22(14):3458-66. [Information]

[4]. Xiaomei Ren, et al. Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway. ACS Med Chem Lett. 2010 Sep 7;1(9):454-9. [Information]

[5]. Chang-Jer Wu, et al. Inhibition of severe acute respiratory syndrome coronavirus replication by niclosamide. Antimicrob Agents Chemother. 2004 Jul;48(7):2693-6. [Information]

溶解度数据

体外研究:

DMF : 5 mg/mL (15.28 mM; Need ultrasonic)

DMSO : 4.55 mg/mL (13.91 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 20% HP-β-CD 5% Cremophor EL
Solubility: 5 mg/mL (15.28 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMF 40% PEG300 5% Tween-80 45% saline
Solubility: 0.5 mg/mL (1.53 mM); Suspended solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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