Tizoxanide

173903-47-4

C10H7N3O4S

265.25

White to off-white powder

Slightly soluble in DMSO and DMF

Source: Synthetic
Purity Level: ≥97% (HPLC)

-20°C

Spectrum: Tizoxanide is effective against parasites (Leishmania mexicana, Trypanosoma cruzi), influenza A, hepatitis B and C. Tizoxanide is active against anaerobic bacteria, protozoa, and a range of viruses. It has both in vitro and in vivo activity against a variety of anaerobic Gram-positive and Gram-negative bacteria as well as aerobic Gram-positive bacteria. It has also been shown to inhibit Mycobacterium tuberculosis.

Microbiology Applications: Nitazoxanide has shown in vitro activity against against SARS-Cov-2. Vero cells were treated wtih Tizoxanide (TIZ) to unveil possible mechanisms for its antimicrobial effect, using a label-free proteomic approach (LC/MS/MS) analysis to compare the proteomic profile between untreated- and TIZ-treated cells. It can lower cell metabolism and RNA processing and modification. The decreased levels of FASN, HNRNPH and HNRNPK with the treatment appear to be important for antiviral activity.

Eukaryotic Cell Culture Applications: The protein binding ability of Tizoxanide in goat plasma, albumin, and alpha-1-acid-glycoprotein were investigated in vitro. The protein binding percentage (at 4 ug/ml) was > 95% in plasma and albumin solution, compared to only 49% in alpha-1-acid-glycoprotein solution, likely due to its acidic property (Zaho et al, 2010). The concept of 'drug repositioning'- using known molecules for new indications, was used to screen 1600 compounds in a high-throughput screening approach using glucose-deprived multicellular tumor spheroids (MCTS) to identify compounds that target dormant cancer cells in solid tumors. Since cancer cells in low glucose environments depend on oxidative phosphorylation rather than solely on glycolysis, continuous exposure is needed, and of the five compounds with MCTS activity, Nitazoxanide is the only one that reaches high plasma concentrations. Nitazoxanide activated the AMPK pathway and down-regulated c-Myc, mTOR, and Wnt signaling, suggesting it could be a candidate for anti-cancer applications (Senkowski W et al, 2015).