Nitazoxanide

別名：NTZ, NSC 697855

製品コード：S1627 純度：99.97%

Nitazoxanide is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent(IC50 for canine influenza virus ranges from 0.17 to 0.21 μM). Nitazoxanide modulates autophagy and inhibits mTORC1 signaling.

CAS No. 55981-09-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
25mg	JPY 22000	国内在庫あり
100mg	JPY 40500	国内在庫あり
1g	JPY 145500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（16）

製品安全説明書

現在のバッチを見る：純度： 99.97%

99.97

Nitazoxanide関連製品

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関連化合物ライブラリー	Anti-infection Compound Library Antibiotics compound Library Antiviral Compound Library Anti-parasitic Compound Library Gut Microbial Metabolite Library	もっと見る

Influenza Virus阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	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
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生物活性

製品説明

Targets

PFOR ^[2]

mTORC1 ^[6]

In Vitro
In vitro	Nitazoxanide reduces parasite growth in cell culture by more than 90% with little evidence of drug-associated cytotoxicity. ^[1] Nitazoxanide is a new thiazolide antiparasitic agent that shows excellent in vitro activity against a wide variety of protozoa and helminths. ^[2] Nitazoxanide and its metabolite tizoxanide are more active in vitro than metronidazole against G. intestinalis, E. histolytica and T. vaginalis. ^[3] Nitazoxanide exhibits potent inhibition of both HBV and HCV replication. Nitazoxanide potentiates the effect of subsequent treatment with Nitazoxanide plus IFN, but not Nitazoxanide plus 2'CmeC, in HCV replicon-containing cells. Nitazoxanide induces reductions in several HBV proteins (HBsAg, HBeAg, HBcAg) produced by 2.2.15 cells, but does not affect HBV RNA transcription. ^[4] Nitazoxanide exhibits IC50, and IC90 values of 0.017 and 0.776 mg/mL respectively, against E. histolytica, 0.004 and 0.067 mg/mL against G. intestinalis, and 0.034 and 2.046 mg/mL against T. vaginalis. Nitazoxanide is more toxic than metronidazole and albendazole against E. histolytica. ^[5]

In Vivo
In Vivo	Nitazoxanide is partially effective at reducing the parasite burden in a gnotobiotic piglet diarrhea model when given orally for 11 days at 250 mg/kg/day but not at 125 mg/kg/day. Nitazoxanide induces a drug-related diarrhea in piglets that might have influenced its therapeutic efficacy. ^[1]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (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

参考
[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

参考

+ 展開

化学情報

分子量	307.28	化学式	C₁₂H₉N₃O₅S
CAS No.	55981-09-4	SDF	Download Nitazoxanide SDFをダウンロードする
Smiles	CC(=O)OC1=CC=CC=C1C(=O)NC2=NC=C(S2)[N+](=O)[O-]
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 61 mg/mL ( (198.51 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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