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Nitazoxanide Influenza Virus Inibitore

N. Cat.: S1627

Nitazoxanide è un derivato sintetico di nitrothiazolil-salicilammide e un agente antiprotozoario (IC50 per il virus dell'influenza canina varia da 0,17 a 0,21 μM). Questo composto modula l'autophagy e inibisce la segnalazione mTORC1.
Nitazoxanide Influenza Virus Inibitore Chemical Structure

Struttura chimica

Peso molecolare: 307.28

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.99%
99.99

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dell'attività PMID
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
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
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
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
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
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
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
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
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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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 307.28 Formula

C12H9N3O5S

Conservazione (Dalla data di ricezione)
N. CAS 55981-09-4 Scarica SDF Conservazione delle soluzioni stock

Sinonimi NTZ, NSC 697855 Smiles CC(=O)OC1=CC=CC=C1C(=O)NC2=NC=C(S2)[N+](=O)[O-]

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 62 mg/mL (201.77 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 62 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa Concentrazione Volume Peso molecolare
Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo
Lotto:

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC50/Ki
PFOR
mTORC1
In vitro

Nitazoxanide reduces parasite growth in cell culture by more than 90% with little evidence of drug-associated cytotoxicity. This compound is a new thiazolide antiparasitic agent that shows excellent in vitro activity against a wide variety of protozoa and helminths. It and its metabolite tizoxanide are more active in vitro than metronidazole against G. intestinalis, E. histolytica and T. vaginalis. This agent exhibits potent inhibition of both HBV and HCV replication. It potentiates the effect of subsequent treatment with this compound plus IFN, but not this chemical plus 2'CmeC, in HCV replicon-containing cells. This chemical induces reductions in several HBV proteins (HBsAg, HBeAg, HBcAg) produced by 2.2.15 cells, but does not affect HBV RNA transcription. It 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. This compound is more toxic than metronidazole and albendazole against E. histolytica.

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. This compound induces a drug-related diarrhea in piglets that might have influenced its therapeutic efficacy.

Riferimenti
  • [4] https://pubmed.ncbi.nlm.nih.gov/17888524/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12120985/
  • [6] https://pubmed.ncbi.nlm.nih.gov/22589723/

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT Reclutamento Condizioni Sponsor/Collaboratori Data di inizio Fasi
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