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

Aller à

Contrôle qualité

Lot : Pureté : 99.99%

99.99

Cibles apparentées	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV
Autre Influenza Virus Inhibiteurs	Arbidol HCl Nucleozin D-Pinitol (-)-Arctigenin Adamantane Cetylpyridinium chloride monohydrate Chebulinic acid

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Temps dincubation	Description de lactivité	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
Cliquez pour voir plus de données expérimentales sur les lignées cellulaires

Informations chimiques, stockage et stabilité

Poids moléculaire	307.28	Formule	C₁₂H₉N₃O₅S	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	55981-09-4	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	NTZ, NSC 697855			Smiles	CC(=O)OC1=CC=CC=C1C(=O)NC2=NC=C(S2)[N+](=O)[O-]

Solubilité

In vitro
Lot:

DMSO : 62 mg/mL (201.77 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 62 mg/mL

Water : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC₅₀/Ki	PFOR mTORC1
In vitro	Le Nitazoxanide réduit la croissance parasitaire en culture cellulaire de plus de 90 % avec peu de preuves de cytotoxicité associée au médicament. Ce composé est un nouvel agent antiparasitaire thiazolide qui présente une excellente activité in vitro contre une grande variété de protozoaires et d'helminthes. Lui et son métabolite, le tizoxanide, sont plus actifs in vitro que le métronidazole contre G. intestinalis, E. histolytica et T. vaginalis. Cet agent exerce une puissante inhibition de la réplication du VHB et du VHC. Il potentialise l'effet d'un traitement ultérieur avec ce composé plus l'IFN, mais pas ce produit chimique plus le 2'CmeC, dans les cellules contenant le réplicon VHC. Ce produit chimique induit des réductions de plusieurs protéines du VHB (AgHBs, AgHBe, AgHBc) produites par les cellules 2.2.15, mais n'affecte pas la transcription de l'ARN du VHB. Il présente des valeurs de CI50 et de CI90 de 0,017 et 0,776 mg/mL respectivement, contre E. histolytica, 0,004 et 0,067 mg/mL contre G. intestinalis, et 0,034 et 2,046 mg/mL contre T. vaginalis. Ce composé est plus toxique que le métronidazole et l'albendazole contre E. histolytica.
In vivo	Le Nitazoxanide est partiellement efficace pour réduire la charge parasitaire dans un modèle de diarrhée de porcelet gnotobiotique lorsqu'il est administré par voie orale pendant 11 jours à 250 mg/kg/jour mais pas à 125 mg/kg/jour. Ce composé induit une diarrhée liée au médicament chez les porcelets qui aurait pu influencer son efficacité thérapeutique.
Références	[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/

Informations sur lessai clinique

(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Sponsor/Collaborateurs	Date de début	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

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

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 inhibiteur

Structure chimique

Poids moléculaire: 307.28