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氯硝柳胺

氯硝柳胺用途

Niclosamide 是一种 STAT3 抑制剂,在 HeLa 细胞中,IC50 值为 0.25 μM,可以抑制 DNA 复制。

氯硝柳胺名称

[ CAS 号 ]:
50-65-7

[ 中文名 ]:
杀螺胺

[ 英文名 ]:
Niclosamide

[中文别名 ]:

[英文别名 ]:

2',5-Dichloro-4'-nitrosalicylanilide
2’,5-dichloro-4’-nitrosalicylanilide
iomesan
nasemo
NICLOCIDE
hl2447
Niclosamide
clonitralid
EINECS 200-056-8
iomezan

氯硝柳胺生物活性

[ 描述 ]:

Niclosamide 是一种 STAT3 抑制剂,在 HeLa 细胞中,IC50 值为 0.25 μM,可以抑制 DNA 复制。

[ 相关类别 ]:

信号通路 >> JAK/STAT信号通路 >> STAT

信号通路 >> 干细胞及 Wnt 通路 >> STAT

研究领域 >> 感染

[ 靶点 ]

STAT3:0.25 μM (IC50, in HeLa cells)

[体外研究]

氯硝柳胺是STAT3的抑制剂,抑制STAT3介导的荧光素酶报告基因活性,在HeLa细胞中IC50为0.25μM。氯硝柳胺(1μM)抑制EGF诱导的Du145细胞中STAT3的核转位。氯硝柳胺(<2μM)剂量依赖性地抑制Du145细胞中STAT3下游基因的转录。氯硝柳胺(<10μM)以剂量依赖的方式诱导Du145癌细胞的G0/G1停滞和凋亡[1]。氯硝柳胺可以在感染SARS-CoV的Vero E6细胞中以微摩尔浓度阻断SARS-CoV复制[2]。氯硝柳胺(<7.5μM)促进Frizzled1内吞作用,下调Disheveled-2蛋白,并抑制Wnt3A刺激的U2OS细胞中β-catenin稳定和LEF/TCF报告基因活性[3]。氯硝柳胺在U2OS细胞中以剂量和时间依赖性方式抑制TNF诱导的NF-κB报告基因活性。氯硝柳胺(125nM)抑制U2OS细胞中p65,IKKα,IKKβ,IKKγ和TAK1诱导的NF-κB活化。氯硝柳胺(<500nM)完全阻断时间和剂量依赖性TNFα诱导的HL-60细胞中NF-κB-DNA复合物的改变。氯硝柳胺(<10nM)抑制U266细胞中的组成型NF-κB活化。氯硝柳胺在HL-60,Molm13或AML原代细胞中以剂量和时间依赖性方式抑制TNF诱导的IκBα降解和p65的重新定位。氯硝柳胺(500nM)引起TNF诱导的NF-κB依赖性基因产物的减少,所述基因产物参与HL-60细胞中的细胞存活。氯硝柳胺还抑制生长并诱导与Mcl-1和XIAP水平降低以及细胞内ROS水平升高相关的AML细胞的强烈凋亡[4]。

[体内研究]

氯硝柳胺(40mg/kg/d,ip)抑制携带HL-60异种移植肿瘤的裸鼠中异种移植的AML细胞的生长[4]。

[激酶实验]

所有蛋白激酶在Sf9昆虫细胞或大肠杆菌中表达为重组GST-融合蛋白或His-标记的蛋白。放射性蛋白激酶测定法用于测量22种蛋白激酶的激酶活性。简而言之，对于每种蛋白激酶，50μL反应混合物含有60mM HEPES-NaOH，3mM MgCl 2,3mM MnCl2,3μM原钒酸钠，1.2mM DTT，50μg/ mLPEG20000,1μM[γ-33P] - ATP，氯硝柳胺，足量的酶及其底物。 PKC-α测定另外含有1mM Ca 2,4mM EDTA，5μg/ mL磷脂酰丝氨酸和1μg/ mL 1,2-二油基甘油。将反应混合物在37℃下孵育60分钟并用50μL2％（v / v）H 3 PO 4终止。用微孔板闪烁计数器测定33Pi的掺入。使用Quattro Workflow V2.28计算活动和IC50值。

[细胞实验]

将细胞接种于96孔培养板中，细胞密度为3-4×103细胞/孔，并在第二天通过加入100μL含有各种浓度的氯硝柳胺的培养基用氯硝柳胺处理。处理72小时后，向每个孔中加入MTT并再孵育4-5小时，并在酶标仪上在570nm处测量吸光度。将细胞生长抑制评估为样品的吸光度与对照的吸光度之比。结果代表至少3次独立实验。

[动物实验]

在测定中使用雄性nu / nu BALB / c小鼠。将HL-60细胞皮下接种在4至6周龄小鼠的侧腹上。每隔一天使用卡尺测量肿瘤。将携带HL-60异种移植物的小鼠随机化以接受用生理盐水（对照）或对氯硝柳胺处理15天（每组n = 7只动物）。肿瘤体积通过下式计算：a2×b×0.4，其中a是最小直径，b是垂直于a的直径。在小鼠实施安乐死后，解剖，称重或保存异种移植物。

[参考文献]

[1]. Ren, X., et al., Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway. ACS Medicinal Chemistry Letters, 2010. 1(9): p. 454-459.

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

[3]. Chen, M., et al., The anti-helminthic niclosamide inhibits Wnt/Frizzled1 signaling. Biochemistry, 2009. 48(43): p. 10267-74.

[4]. Jin, Y., et al. Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-kappaB pathway and generation of reactive oxygen species. Cancer Res, 2010. 70(6): p. 2516-27.

[相关活性小分子]

氯硝柳胺物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
424.5±45.0 °C at 760 mmHg

[ 熔点 ]:
225-230ºC

[ 分子式 ]:
C₁₃H₈Cl₂N₂O₄

[ 分子量 ]:
327.120

[ 闪点 ]:
210.5±28.7 °C

[ 精确质量 ]:
325.986115

[ PSA ]:
95.15000

[ LogP ]:
5.41

[ 外观性状 ]:
白色至淡黄色无臭结晶粉末

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.709

[ 储存条件 ]:
库房通风低温干燥,与食品原料分开储运

氯硝柳胺MSDS

详细MSDS(安全技术说明书)

氯硝柳胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VN8400000

CHEMICAL NAME :: Salicylanilide, 2',5-dichloro-4'-nitro-

CAS REGISTRY NUMBER :: 50-65-7

LAST UPDATED :: 199712

DATA ITEMS CITED :: 17

MOLECULAR FORMULA :: C13-H8-Cl2-N2-O4

MOLECULAR WEIGHT :: 327.13

WISWESSER LINE NOTATION :: WNR CG DMVR BQ EG

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 250 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7500 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 300 mg/kg

SEX/DURATION :: male 5 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Sister chromatid exchange

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 300 mg/kg/5D (Continuous)

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 204,269,1988

氯硝柳胺安全信息

[ 符号 ]:

GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H400

[ 警示性声明 ]:
P273

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
UN 3077 9/PG 3

[ WGK德国 ]:
2

[ RTECS号 ]:
VN8400000

[ 危险类别 ]:
9.0

[ 海关编码 ]:
2924299090

氯硝柳胺制备

1.2-氯-4-硝基苯胺与5-氯水杨酸以等摩尔比溶于二甲苯（或氯苯）中，沸腾下慢慢加入三氯化磷（或三氯氧磷），加毕，继续回流3h，冷却，滤出结晶即为氯硝柳胺。

氯硝柳胺海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

氯硝柳胺文献

The salicylanilide derivatives inhibit signal transducer and activator of transcription 3 pathways in A549 lung cancer cells.

Anticancer Drugs 27 , 41-7, (2015)

The signal transducer and activator of transcription 3 (STAT3) is constitutively activated in certain cancer cells. Therefore, blocking the aberrant activity of STAT3 in tumor cells is a validated the...

Taenia solium: Development of an Experimental Model of Porcine Neurocysticercosis.

PLoS Negl. Trop. Dis. 9 , e0003980, (2015)

Human neurocysticercosis (NC) is caused by the establishment of Taenia solium larvae in the central nervous system. NC is a severe disease still affecting the population in developing countries of Lat...

Phase I and phase II reductive metabolism simulation of nitro aromatic xenobiotics with electrochemistry coupled with high resolution mass spectrometry.

Anal. Bioanal. Chem 406(28) , 7253-60, (2014)

Electrochemistry combined with (liquid chromatography) high resolution mass spectrometry was used to simulate the general reductive metabolism of three biologically important nitro aromatic molecules:...

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