Niclosamide

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Niclosamide

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

50-65-7

氯硝柳胺
BAY2353

Niclosamide (BAY2353) 是一种具有口服活性的用于寄生虫感染研究的抗蠕虫化合物。Niclosamide 是STAT3抑制剂，在 HeLa 细胞中的IC₅₀为 0.25 μM。Niclosamide 具有抗癌的生物活性，并能抑制 Vero E6 细胞的 DNA 复制。

生物活性

Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasiticinfectionresearch^[1]. Niclosamide is aSTAT3inhibitor with anIC₅₀of 0.25 μM in HeLa cells^[4]. Niclosamide has biological activities againstcancer, inhibits DNA replication in Vero E6 cells^[2]^[3]^[5].

IC₅₀& Target

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^[3].
Niclosamide (0.05-5 μM, 24 h) treatment inhibits STAT3-mediated luciferase reporter activity in HeLa cells^[4].
Niclosamide (10 μM) treatment inhibits virus replication in Vero E6 cells^[5].

Cell Viability Assay^[3]

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 IC₅₀of 0.12 μM, 0.15 μM, and 0.53 μM in BD140A, SW-13, and NCI-H295R, respectively.

Cell Viability Assay^[4]

Cell Line:	Hela cells
Concentration:	0.05-5 μM
Incubation Time:	24 hours
Result:	Inhibited STAT3-mediated luciferase reporter activity with an IC₅₀of 0.25 μM.

Cell Viability Assay^[4]

Cell Line:	Vero E6 cells^[5]
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^[3].

Animal Model:	Nu⁺/Nu⁺mice injected with NCI-H295R cells^[3]
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.

Clinical Trial

分子量

327.12

性状

Solid

Formula

C₁₃H₈Cl₂N₂O₄

CAS 号

50-65-7

中文名称

氯硝柳胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

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℃)(insoluble)

配制储备液

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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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.
请依序添加每种溶剂： 20%HP-β-CD 5% Cremophor EL
Solubility: 5 mg/mL (15.28 mM); Suspended solution; Need ultrasonic
2.
请依序添加每种溶剂： 10% DMF 40%PEG300 5%Tween-80 45% saline
Solubility: 0.5 mg/mL (1.53 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。