solo per uso di ricerca
N. Cat.: S1627
Struttura chimica
| Target correlati | Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV |
|---|---|
| Altro Influenza Virus Inibitori | Arbidol HCl Nucleozin Cetylpyridinium chloride monohydrate D-Pinitol (-)-Arctigenin Adamantane Chebulinic acid |
| 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 | |||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
| Peso molecolare | 307.28 | Formula | C12H9N3O5S |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 55981-09-4 | Scarica SDF | Conservazione delle soluzioni stock |
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| Sinonimi | NTZ, NSC 697855 | Smiles | CC(=O)OC1=CC=CC=C1C(=O)NC2=NC=C(S2)[N+](=O)[O-] | ||
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In vitro |
DMSO
: 62 mg/mL
(201.77 mM)
Ethanol : 62 mg/mL Water : Insoluble |
|
In vivo |
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Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)
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.)
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.
| 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 |
|
(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 |