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Nitazoxanide
别名: NTZ, NSC 697855 中文名称：硝唑尼特
Nitazoxanide是一种人工合成的nitrothiazolyl-salicylamide衍生物，是一种抗原虫剂（作用于犬流感病毒，IC50为0.17 到0.21 μM）。Nitazoxanide 可调节自噬并抑制 mTORC1 信号传递。
Nitazoxanide Chemical Structure
CAS: 55981-09-4
产品质控
批次：
纯度：
99.97%
99.97
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息(PMID) |
|---|---|---|---|---|---|
| Ava5 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1b infected in Ava5 cells assessed as inhibition of viral replication after 3 days by blot hybridization analysis, EC50=0.21μM | 22059983 | |
| Huh7.5 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1a infected in Huh7.5 cells assessed as inhibition of viral replication after 3 days by blot hybridization analysis, EC50=0.33μM | 22059983 | |
| Ava5 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1b infected in Ava5 cells assessed as inhibition of viral replication after 3 days by blot hybridization analysis, EC90=0.93μM | 22059983 | |
| Huh7.5 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1a infected in Huh7.5 cells assessed as inhibition of viral replication after 3 days by blot hybridization analysis, EC90=1.1μM | 22059983 | |
| HCT8 | Antiparasitic assay | 48 hrs | Antiparasitic activity against Cryptosporidium parvum SPL infected in human HCT8 cells incubated for 48 hrs by FITC/DAPI staining based fluorescence assay, EC50=2.3μM | 29469575 | |
| Vero E6 | Function assay | 48 hrs | IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells), IC50=2.81838μM | 32353859 | |
| HCT8 | Antiparasitic assay | 48 hrs | Antiparasitic activity against Cryptosporidium parvum BGF infected in human HCT8 cells incubated for 48 hrs by FITC/DAPI staining based fluorescence assay, EC50=2.9μM | 29469575 | |
| Vero | Cytotoxicity assay | 48 hrs | Cytotoxicity against african green monkey Vero cells assessed as cell viability after 48 hrs by WST-1 assay, IC50=10.74μM | 23787289 | |
| BHK21 | Cytotoxicity assay | 16 hrs | Cytotoxicity against BHK21 cells assessed as reduction in cell viability after 16 hrs by CCK-8 assay, CC50=25μM | 28689975 | |
| U2OS | Cytotoxicity assay | 16 hrs | Cytotoxicity against human U2OS cells assessed as reduction in cell viability after 16 hrs by CCK-8 assay, CC50=25μM | 28689975 | |
| Ava5 | Cytotoxicity assay | 3 days | Cytotoxicity against human Ava5 cells after 3 days by neutral red dye assay, CC50=35μM | 22059983 | |
| Huh7.5 | Cytotoxicity assay | 3 days | Cytotoxicity against human Huh7.5 cells after 3 days by neutral red dye assay, CC50=49μM | 22059983 | |
| HepG2(2.2.15) | Antiviral assay | Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in extracellular viral DNA measured 24 hrs after last dose, EC50=0.12μM | 21553812 | ||
| HepG2(2.2.15) | Antiviral assay | Antiviral activity against HBV infected in human HepG2(2.2.15) cells assessed as inhibition of extracellular viral DNA level, IC50=0.12μM | 28383274 | ||
| HepG2(2.2.15) | Antiviral assay | Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in intracellular viral DNA measured 24 hrs after last dose, EC50=0.59μM | 21553812 | ||
| HepG2(2.2.15) | Antiviral assay | Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in extracellular viral DNA measured 24 hrs after last dose, EC90=0.83μM | 21553812 | ||
| BHK-21 | Antiviral assay | Antiviral activity against Chikungunya virus 0611aTw infected in BHK-21 cells by RT-qPCR analysis, EC50=1.96μM | 28689975 | ||
| HepG2(2.2.15) | Antiviral assay | Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in intracellular viral DNA measured 24 hrs after last dose, EC90=2.1μM | 21553812 | ||
| BHK-21 | Antiviral assay | Antiviral activity against Chikungunya virus infected in BHK-21 cells by RT-qPCR analysis, EC50=2.96μM | 28689975 | ||
| U2OS | Antiviral assay | Antiviral activity against Chikungunya virus infected in human U2OS cells by RT-qPCR analysis, EC50=3.01μM | 28689975 | ||
| HCT8 | Antiparasitic assay | Antiparasitic activity against Cryptosporidium parvum in HCT8 cells, IC50=3.25μM | 16480281 | ||
| HCT-8 | Antimicrobial assay | Antimicrobial activity against Cryptosporidium parvum infected in human HCT-8 cells, IC50=3.8μM | 18591280 | ||
| BHK-21 | Antiviral assay | Antiviral activity against Chikungunya virus 0810bTw infected in BHK-21 cells by RT-qPCR analysis, EC50=4.95μM | 28689975 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Nitazoxanide是一种人工合成的nitrothiazolyl-salicylamide衍生物，是一种抗原虫剂（作用于犬流感病毒，IC50为0.17 到0.21 μM）。Nitazoxanide 可调节自噬并抑制 mTORC1 信号传递。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在细胞培养物中，Nitazoxanide降低90％以上的寄生虫的生长，没有人和药物相关的细胞毒性迹象。[1] Nitazoxanide是一种新的thiazolide寄生虫驱除剂，显示优异的对多种原生动物和蠕虫的体外活性。[2] Nitazoxanide及其代谢物tizoxanide在体外比甲硝唑对G. intestinalis, E. histolytica和T. vaginalis有更强的活性。[3] Nitazoxanide表现出对HBV和HCV复制的有效抑制。在HCV的复制子含有细胞中，Nitazoxanide使后续用Nitazoxanide加上干扰素处理更为有效，但不增强Nitazoxanide加上2'CmeC的效果。Nitazoxanide诱导几个HBV蛋白（HBsAg和HBeAg的，核心抗原）在2.2.15细胞中产生的减少，但不影响HBV的RNA的转录。[4] Nitazoxanide表现出对E. histolytica的IC50和IC90值分别为0.017 mg/mL和0.776 mg/mL，对G. intestinalis分别使0.004 mg/mL和0.067 mg/mL，对T. vaginalis.分别为0.034 mg/mL和2.046 mg/mL。Nitazoxanide比甲硝唑和丙硫咪唑对溶组织内阿米巴毒性更大。[5] |
|||
|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在一个无菌幼猪腹泻模型中，Nitazoxanide（250 mg/kg）口服处理11天后，降低了寄生虫的数量。Nitazoxanide诱导了一个药物相关的腹泻可能影响了它的治疗效果。 [1] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06049901 | Recruiting | Metastatic Colorectal Cancer |
Tanta University |
March 1 2023 | Phase 3 |
| NCT05701423 | Recruiting | Multiple Sclerosis |
Biogen |
February 8 2023 | -- |
| NCT05368935 | Completed | Renal Impairment|Renal Disease|Kidney Disease |
Genfit |
April 25 2022 | Phase 1 |
| NCT05116826 | Completed | Moderate Hepatic Impairment|Severe Hepatic Impairment|Liver Diseases |
Genfit |
November 5 2021 | Phase 1 |
| NCT03656068 | Completed | Non-alcoholic Steatohepatitis|Fatty Liver|Fibrosis Liver|Compensated Cirrhosis |
Pinnacle Clinical Research PLLC |
December 4 2018 | Phase 2 |
| NCT02684240 | Completed | Tuberculosis |
Weill Medical College of Cornell University |
February 2016 | Phase 2 |
|
化学信息&溶解度
| 分子量 | 307.28 | 分子式 | C12H9N3O5S |
| CAS号 | 55981-09-4 | SDF | Download Nitazoxanide SDF |
| Smiles | CC(=O)OC1=CC=CC=C1C(=O)NC2=NC=C(S2)[N+](=O)[O-] | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 61 mg/mL ( (198.51 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
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）
mg/kg
g
μL
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Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
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，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
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 ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：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。
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