Nitazoxanide

Catalog No.S1627

Nitazoxanide is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent. (IC50 for canine influenza virus ranges from 0.17 to 0.21 μM)

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Nitazoxanide Chemical Structure

Nitazoxanide Chemical Structure
Molecular Weight: 307.28

Validation & Quality Control

MSDS

Related Compound Libraries

Nitazoxanide is available in the following compound libraries:

Product Information

Product Description

Biological Activity

Description Nitazoxanide is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent. (IC50 for canine influenza virus ranges from 0.17 to 0.21 μM)
Targets PFOR [2]
In vitro Nitazoxanide reduces parasite growth in cell culture by more than 90% with little evidence of drug-associated cytotoxicity. [1] Nitazoxanide is a new thiazolide antiparasitic agent that shows excellent in vitro activity against a wide variety of protozoa and helminths. [2] Nitazoxanide and its metabolite tizoxanide are more active in vitro than metronidazole against G. intestinalis, E. histolytica and T. vaginalis. [3] Nitazoxanide exhibits potent inhibition of both HBV and HCV replication. Nitazoxanide potentiates the effect of subsequent treatment with Nitazoxanide plus IFN, but not Nitazoxanide plus 2'CmeC, in HCV replicon-containing cells. Nitazoxanide induces reductions in several HBV proteins (HBsAg, HBeAg, HBcAg) produced by 2.2.15 cells, but does not affect HBV RNA transcription. [4] Nitazoxanide 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. Nitazoxanide is more toxic than metronidazole and albendazole against E. histolytica. [5]
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. Nitazoxanide induces a drug-related diarrhea in piglets that might have influenced its therapeutic efficacy. [1]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Theodos CM, et al. Antimicrob Agents Chemother, 1998, 42(8), 1959-1965.

[2] Fox LM, et al. Clin Infect Dis, 2005, 40(8), 1173-1180.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-04-18)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02334163 Recruiting Hepatic Encephalopathy Ain Shams University|Al-Azhar University December 2014 Phase 2
NCT02165813 Recruiting Gastroenteritis Telethon Kids Institute|The University of Western Austral  ...more Telethon Kids Institute|The University of Western Australia|Menzies School of Health Research November 2014 Phase 2
NCT02057757 Recruiting Severe Acute Respiratory Illness National Institute of Allergy and Infectious Diseases (NI  ...more National Institute of Allergy and Infectious Diseases (NIAID)|Mexican Emerging Infectious Diseases Clinical Research Network (La Red) February 2014 Phase 2
NCT01610245 Completed Influenza Romark Laboratories L.C. March 2013 Phase 3
NCT01559636 Withdrawn Poliomyelitis Seroconversion|Diarrhea Centers for Disease Control and Prevention|Tribhuvan Univ  ...more Centers for Disease Control and Prevention|Tribhuvan University, Nepal May 2012 Phase 3

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Chemical Information

Download Nitazoxanide SDF
Molecular Weight (MW) 307.28
Formula

C12H9N3O5S

CAS No. 55981-09-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 62 mg/mL (201.77 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-​(acetyloxy)​-​N-​(5-​nitro-​2-​thiazolyl)​-benzamide

Research Area

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