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Nitazoxanide Influenza Virus Inhibitor

Kat.-Nr.: S1627

Nitazoxanide ist ein synthetisches Nitrothiazolyl-Salicylamid-Derivat und ein Antiprotozoenmittel (IC50 für das canine Influenza Virus liegt zwischen 0,17 und 0,21 μM). Diese Verbindung moduliert die Autophagy und hemmt die mTORC1-Signalgebung.
Nitazoxanide Influenza Virus Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 307.28

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Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.99%
99.99

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung 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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Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 307.28 Formel

C12H9N3O5S

 Lagerung (Ab Erhaltdatum)
CAS-Nr. 55981-09-4 SDF herunterladen Lagerung von Stammlösungen

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

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 62 mg/mL (201.77 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 62 mg/mL

Water : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewicht-Rechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie unten die Informationen ein (Empfohlen: Ein zusätzliches Tier einplanen, um Verluste während des Experiments auszugleichen)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, nicht die Formulierung. Bitte kontaktieren Sie uns zuerst, wenn im Abschnitt Löslichkeit keine In-vivo-Formulierung angegeben ist.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammflüssigkeit: mg Wirkstoff voraufgelöst in μL DMSO ( Konzentration der Stammflüssigkeit mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der jeweiligen Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzuμL PEG300, mischen und aufklären, fügen Sie als Nächstes hinzuμL Tween 80, mischen und aufklären, fügen Sie als Nächstes hinzu μL ddH2O, mischen und aufklären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzu μL Maisöl, mischen und aufklären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, die Lösungsmittel in der richtigen Reihenfolge hinzuzufügen. Sie müssen sicherstellen, dass die im vorherigen Schritt erhaltene Lösung klar ist, bevor Sie das nächste Lösungsmittel hinzufügen. Physikalische Methoden wie Vortexen, Ultraschall oder ein warmes Wasserbad können zur Unterstützung des Lösungsvorgangs verwendet werden.

Wirkungsmechanismus (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.

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

Informationen zu klinischen Studien (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Bedingungen Sponsor/Kollaboratoren Startdatum 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