Name: Nitazoxanide
Brand: Selleck Chemicals
SKU: S1627
Rating: 5 (19 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV
Overig Influenza Virus Inhibitoren	Arbidol HCl Nucleozin Cetylpyridinium chloride monohydrate D-Pinitol (-)-Arctigenin Adamantane Chebulinic acid

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Incubatietijd	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	307.28	Formule	C₁₂H₉N₃O₅S	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	55981-09-4	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NTZ, NSC 697855			Smiles	CC(=O)OC1=CC=CC=C1C(=O)NC2=NC=C(S2)[N+](=O)[O-]

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 62 mg/mL (201.77 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 62 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.500mg/ml (4.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.000mg/ml (3.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	PFOR mTORC1
In vitro	Nitazoxanide vermindert de parasietgroei in celkweken met meer dan 90% met weinig bewijs van geneesmiddelgerelateerde cytotoxiciteit. Deze verbinding is een nieuw thiazolide antiparasitair middel dat uitstekende in vitro activiteit vertoont tegen een breed scala aan protozoa en helminths. Het en zijn metaboliet tizoxanide zijn in vitro actiever dan metronidazol tegen G. intestinalis, E. histolytica en T. vaginalis. Dit middel vertoont een potente remming van zowel HBV- als HCV-replicatie. Het versterkt het effect van daaropvolgende behandeling met deze verbinding plus IFN, maar niet dit chemische middel plus 2'CmeC, in HCV-replicon-bevattende cellen. Dit chemische middel induceert reducties in verschillende HBV-eiwitten (HBsAg, HBeAg, HBcAg) geproduceerd door 2.2.15-cellen, maar heeft geen invloed op de HBV RNA-transcriptie. Het vertoont IC50- en IC90-waarden van respectievelijk 0,017 en 0,776 mg/mL tegen E. histolytica, 0,004 en 0,067 mg/mL tegen G. intestinalis, en 0,034 en 2,046 mg/mL tegen T. vaginalis. Deze verbinding is toxischer dan metronidazol en albendazol tegen E. histolytica.
In vivo	Nitazoxanide is gedeeltelijk effectief in het verminderen van de parasietbelasting in een gnotobiotisch biggen diarree model wanneer oraal toegediend gedurende 11 dagen met 250 mg/kg/dag, maar niet met 125 mg/kg/dag. Deze verbinding induceert een geneesmiddelgerelateerde diarree bij biggen die mogelijk de therapeutische werkzaamheid heeft beïnvloed.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/9687390/ [2] https://pubmed.ncbi.nlm.nih.gov/15791519/ [3] https://pubmed.ncbi.nlm.nih.gov/11751773/ [4] https://pubmed.ncbi.nlm.nih.gov/17888524/ [5] https://pubmed.ncbi.nlm.nih.gov/12120985/ [6] https://pubmed.ncbi.nlm.nih.gov/22589723/

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Nitazoxanide Influenza Virus inhibitor

Chemische structuur

Molecuulgewicht: 307.28

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie over klinische proeven (Clinical Trial Information)

Nitazoxanide Influenza Virus inhibitor

Chemische structuur

Molecuulgewicht: 307.28

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie over klinische proeven (Clinical Trial Information)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)