Nitazoxanide

SKU: orb1224663

Description

Nitazoxanide, also known by the brand name Alinia, is a synthetic nitrothiazolyl-salicylamide derivative and an anti-protozoal agent. It is approved for treatment of infectious diarrhea caused by Cryptosporidium parvum and Giardia lamblia in patients 1 year of age and older. Following oral administration it is rapidly hydrolyzed to its active metabolite, tizoxanide, which is 99% protein bound. Peak concentrations are observed 1-4 hours after administration. It is excreted in the urine, bile and feces. Untoward effects include abdominal pain, vomiting and diarrhea. (In Vitro):Giardia lamblia, a flagellated protozoan, is the most common causative agent of persistent diarrhea worldwide.Nitazoxanide exhibits effect on G. lamblia trophozoite proliferation in axenic culture with an IC50 of 2.4 μM.(In Vivo):Nitazoxanide exhibits a wide spectrum of in vivo activity against a broad spectrum of intestinal parasites, such as Giardia lamblia, Entamoeba histolytica, Trichomonas vaginalis, the apicomplexan Cryptosporidium parvum, and enteric bacteria infecting animals and humans.Nitazoxanide (50, 75 or 100 mg/kg/day; administered daily by intragastric for up to 25 days) reduces the mortality of Japanese encephalitis virus (JEV) strain-infected mice and protected mice from a lethal dose challenge of JEV.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 55981-09-4
• MW: 307.28
• Purity: >98% (HPLC)
• Formula: C₁₂H₉N₃O₅S
• SMILES: CC(OC1=CC=CC=C1C(NC2=NC=C([N+]([O-])=O)S2)=O)=O
• Target: PFOR
• Solubility: DMSO: 62 mg/mL (201.77 mM)

Bioactivity

• In Vivo:
  Nitazoxanide exhibits a wide spectrum of In vivo activity against a broad spectrum of intestinal parasites, such as Giardia lamblia, Entamoeba histolytica, Trichomonas vaginalis, the apicomplexan Cryptosporidium parvum, and enteric bacteria infecting animals and humans. Nitazoxanide (50, 75 or 100 mg/kg/day; administered daily by intragastric for up to 25 days) reduces the mortality of Japanese encephalitis virus (JEV) strain-infected mice and protected mice from a lethal dose challenge of JEV. Animal model: Three-week old female Chinese Kunming mice (12–14 g body weight) were infected intraperitoneally with JEV. Dosage: 50, 75 or 100 mg/kg/day. Administration: Administered intragastrically by gavage. Result: 50 mg/kg/day, 75 mg/kg/day and 100 mg/kg/day led to 30%, 70% and 90% mice survival, respectively.
• In Vitro:
  Giardia lamblia, a flagellated protozoan, is the most common causative agent of persistent diarrhea worldwide. Nitazoxanide exhibits effect on G. lamblia trophozoite proliferation in axenic culture with an IC50 of 2.4 μM. Cell Viability Assay Cell line: Human cancer colon Caco2 cells were incubated with increasing numbers of Giardia lamblia trophozoites (103 to 106 parasites per well). Concentration: 30 μM. Incubation time: 24 hours. Result: 70 to 90% of the trophozoites remained attached to the Caco2 cells for a period of 24 to 48 h in the absence of Nitazoxanide and at an initial inoculum density of 105 parasites per well. The number of parasites still attached to Caco2 cells after 24 h decreased to less than 20% of the control value in the presence of 30 μM Nitazoxanide with an inoculum density of 105 trophozoites.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NSC 697855 | NTZ

Quick Database Links

Gene Symbol

PFOR