Nitazoxanide

別名: NTZ, NSC 697855 中文名稱：硝唑尼特

目錄號：S1627 Purity: 99.97%

Nitazoxanide是一種人工合成的nitrothiazolyl-salicylamide衍生物，是一種抗原蟲劑（作用于犬流感病毒，IC50為0.17 到0.21 μM）。Nitazoxanide 可調(diào)節(jié)自噬并抑制 mTORC1 信號傳遞。

Nitazoxanide Chemical Structure

CAS: 55981-09-4

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1072.67	現(xiàn)貨
25mg	812.74	現(xiàn)貨
100mg	2233.86	現(xiàn)貨
1g	7944.3	現(xiàn)貨
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400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.97%

99.97

Nitazoxanide相關產(chǎn)品

相關產(chǎn)品	Nucleozin	點擊展開
相關化合物庫	抗感染化合物庫抗生素化合物庫抗病毒化合物庫抗寄生蟲藥物庫腸道微生物代謝物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	孵育時間	活性描述	文獻信息
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點

PFOR ^[2]

mTORC1 ^[6]

體外研究(In Vitro)
體外研究活性	在細胞培養(yǎng)物中，Nitazoxanide降低90％以上的寄生蟲的生長，沒有人和藥物相關的細胞毒性跡象。^[1] Nitazoxanide是一種新的thiazolide寄生蟲驅(qū)除劑，顯示優(yōu)異的對多種原生動物和蠕蟲的體外活性。^[2] Nitazoxanide及其代謝物tizoxanide在體外比甲硝唑?qū). intestinalis, E. histolytica和T. vaginalis有更強的活性。^[3] Nitazoxanide表現(xiàn)出對HBV和HCV復制的有效抑制。在HCV的復制子含有細胞中，Nitazoxanide使后續(xù)用Nitazoxanide加上干擾素處理更為有效，但不增強Nitazoxanide加上2'CmeC的效果。Nitazoxanide誘導幾個HBV蛋白（HBsAg和HBeAg的，核心抗原）在2.2.15細胞中產(chǎn)生的減少，但不影響HBV的RNA的轉(zhuǎn)錄。^[4] Nitazoxanide表現(xiàn)出對E. histolytica的IC50和IC90值分別為0.017 mg/mL和0.776 mg/mL，對G. intestinalis分別使0.004 mg/mL和0.067 mg/mL，對T. vaginalis.分別為0.034 mg/mL和2.046 mg/mL。Nitazoxanide比甲硝唑和丙硫咪唑?qū)θ芙M織內(nèi)阿米巴毒性更大。^[5]

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在一個無菌幼豬腹瀉模型中，Nitazoxanide（250 mg/kg）口服處理11天后，降低了寄生蟲的數(shù)量。Nitazoxanide誘導了一個藥物相關的腹瀉可能影響了它的治療效果。 ^[1]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻
[1] Theodos CM, et al. Antimicrob Agents Chemother, 1998, 42(8), 1959-1965. [2] Fox LM, et al. Clin Infect Dis, 2005, 40(8), 1173-1180. [3] Adagu IS, et al. J Antimicrob Chemother, 2002, 49(1), 103-111. [4] Korba BE, et al. Antiviral Res, 2008, 77(1), 56-63. [5] Cedillo-Rivera R, et al. J Eukaryot Microbiol, 2002, 49(3), 201-208. [6] Karen K Y Lam, et al. PLoS Pathog . 2012;8(5):e1002691. + 展開

參考文獻

[1] Theodos CM, et al. Antimicrob Agents Chemother, 1998, 42(8), 1959-1965.
[2] Fox LM, et al. Clin Infect Dis, 2005, 40(8), 1173-1180.
[3] Adagu IS, et al. J Antimicrob Chemother, 2002, 49(1), 103-111.

[4] Korba BE, et al. Antiviral Res, 2008, 77(1), 56-63.
[5] Cedillo-Rivera R, et al. J Eukaryot Microbiol, 2002, 49(3), 201-208.
[6] Karen K Y Lam, et al. PLoS Pathog . 2012;8(5):e1002691.

+ 展開

化學信息&溶解度

分子量	307.28	分子式	C₁₂H₉N₃O₅S
CAS號	55981-09-4	SDF	Download Nitazoxanide SDF
Smiles	CC(=O)OC1=CC=CC=C1C(=O)NC2=NC=C(S2)[N+](=O)[O-]
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 61 mg/mL ( (198.51 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 62 mg/mL ( (201.77 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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