Tizoxanide|173903-47-4|(替唑尼特; TIZ)-陌孚医药/Medlife

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Tizoxanide (Synonyms: 替唑尼特; TIZ)

目录号: PC12983 纯度: ≥98%

CAS No. :173903-47-4

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中文名称

Tizoxanide

中文别名

N2-(1-乙氧羰基-3-苯丙基)-N6-三氟乙酰基-L-赖氨酸;Tizoxanide(硝唑尼特杂质C);替唑尼特;2-羟基-N-(5-硝基-2-噻唑基)苯甲酰胺;脱乙酰基-D4;TIZOXANIDE(替唑尼特);2-羟基-N-(5-硝基噻唑-2-基)苯甲酰胺

英文名称

Tizoxanide

英文别名

TIZOXANIDE;TIZ;2-Hydroxy-N-(5-nitro-2-thiazolyl)benzamide;Desacetylnitazoxanide;NTZdes;NSC 697856;2-hydroxy-N-(5-nitrothiazol-2-yl)benzaMide;Benzamide, 2-hydroxy-N-(5-nitro-2-thiazolyl)-;Desacetyl-nitazoxanide;15KFG88UOJ;2-hydroxy-N-(5-nitro-1,3-thiazol-2-yl)benzamide;NSC697856;C10H7N3O4S;PubChem20794;BCP08678;8987AA;NE62763;N-(5-nitro

Cas No.

173903-47-4

分子式

C₁₀H₇N₃O₄S

分子量

265.25

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

Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC₅₀ of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells.

性状

Solid

IC50 & Target[1][2]

Tizoxanide (TIZ) has potent inhibition of both HBV and HCV replication with values EC₅₀ of 0.46μM and 0.15 μM, respectively.

体外研究(In Vitro)

Tizoxanide (TIZ) induces mild mitochondrial uncoupling and activate AMPK in hepatocytes.
Tizoxanide (TIZ) inhibits hepatitis C virus (HCV) replication in HCV replicon systems.

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

Cell Viability Assay

Cell Line:	HepG2 cells
Concentration:	1-25 μmol/L
Incubation Time:	24 h
Result:	Induced mitochondrial uncoupling and AMPK activation not due to the non-specific cytotoxicity in HepG2 cells at concentrations less than 25 μmol/L.

Immunofluorescence

Cell Line:	HepG2 cells
Concentration:	10 μmol/L
Incubation Time:	24 h
Result:	Promoted the nuclear translocation of TFEB by activating AMPK in HepG2 cells.

RT-PCR

Cell Line:	HepG2 cells
Concentration:	1-25 μmol/L
Incubation Time:	24 h
Result:	Induced the increase transcription of SQSTM1/P62 in HepG2 cells.

Western Blot Analysis

Cell Line:	HepG2 cells
Concentration:	1-25 μmol/L
Incubation Time:	24 h
Result:	Activated AMPK and increased phosphorylation of ACC in HepG2 cells.

Cell Cytotoxicity Assay

Cell Line:	RP7 cells, NTZ-11 and TIZ-9 cell lines
Concentration:	The initial drug concentration was 0.02 μM, followed by 0.05, 0.1, 0.5, and 1 μM, and subsequent weekly increases of 1 μM until a final concentration of 11 μM.
Incubation Time:	3 days
Result:	Againsted HCV replication in RP7 cells (IC₅₀: 0.16), NTZ-11 (IC₅₀:1.2) and TIZ-9 cell lines (IC₅₀: 1.5)

体内研究(In Vivo)

Tizoxanide (TIZ) (10 mg/kg; i.v.) can pass the BBB and distribute to the brain tissue. Tizoxanide retains in brain is obviously longer than that in plasma.

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

Animal Model:	Sprague Dawley rats
Dosage:	10 mg/kg
Administration:	Tizoxanide (10 mg/kg; i.v.)
Result:	Could pass the BBB and distribute to the brain tissue.

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

参考文献

[1]. Fengfeng Li, et al. Anthelmintics nitazoxanide protects against experimental hyperlipidemia and hepatic steatosis in hamsters and mice. Acta Pharm Sin B. 2022 Mar;12(3):1322-1338. [Information]

[2]. Sixun Guo, et al. Analysis of tizoxanide, active metabolite of nitazoxanide, in rat brain tissue and plasma by UHPLC-MS/MS. Biomed Chromatogr. 2020 Feb;34(2):e4716. [Information]

[3]. Brent E Korba, et al. Potential for hepatitis C virus resistance to nitazoxanide or tizoxanide. Antimicrob Agents Chemother. 2008 Nov;52(11):4069-71. [Information]

[4]. Brent E Korba, et al. Nitazoxanide, tizoxanide and other thiazolides are potent inhibitors of hepatitis B virus and hepatitis C virus replication. [Information]

[5]. Jiaoqin Shou, et al. Tizoxanide Inhibits Inflammation in LPS-Activated RAW264.7 Macrophages via the Suppression of NF-κB and MAPK Activation. Inflammation. 2019 Aug;42(4):1336-1349. [Information]

[6]. Korba BE, et al. Nitazoxanide, tizoxanide and other thiazolides are potent inhibitors of hepatitis B virus and hepatitis C virus replication. Antiviral Res. 2008 Jan;77(1):56-63. [Information]

[7]. Korba BE, et al. Potential for hepatitis C virus resistance to nitazoxanide or tizoxanide. Antimicrob Agents Chemother. 2008 Nov;52(11):4069-71. [Information]

[8]. Ashton LV, et al. 体外研究 Susceptibility of Canine Influenza A (H3N8) Virus to Nitazoxanide and Tizoxanide. Vet Med Int. 2010 Aug 12;2010. pii: 891010. [Information]

[9]. Trabattoni D, et al. Thiazolides Elicit Anti-Viral Innate Immunity and Reduce HIV Replication. Sci Rep. 2016 Jun 2;6:27148. [Information]

溶解度数据

体外研究:

DMSO : ≥ 38 mg/mL (143.26 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7700 mL	18.8501 mL	37.7003 mL
5 mM	0.7540 mL	3.7700 mL	7.5401 mL
10 mM	0.3770 mL	1.8850 mL	3.7700 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。

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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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