1. Anti-infection Autophagy NF-κB
  2. Bacterial HIV Autophagy Parasite IKK Influenza Virus
  3. Tizoxanide

Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC50 of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells.

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Tizoxanide Chemical Structure

Tizoxanide Chemical Structure

CAS No. : 173903-47-4

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Customer Review

Based on 10 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC50 of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells[1][3][4][5].

IC50 & Target

HIV-1

 

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
29.8 μM
Compound: TIZ
Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay
[PMID: 34055214]
HepG2 2.2.15 CC50
> 100 μM
Compound: 2
Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red dye uptake assay
Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red dye uptake assay
[PMID: 21553812]
Huh-7 CC50
14 μM
Compound: 2
Cytotoxicity against human Huh7.5 cells after 3 days by neutral red dye assay
Cytotoxicity against human Huh7.5 cells after 3 days by neutral red dye assay
[PMID: 22059983]
Vero CC50
388 μM
Compound: Tizoxanide
Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay
[PMID: 25801157]
Vero CC50
388 μM
Compound: TIZ
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay
[PMID: 21397502]
In Vitro

Tizoxanide (TIZ) induces mild mitochondrial uncoupling and activate AMPK in hepatocytes[1].
Tizoxanide (TIZ) inhibits hepatitis C virus (HCV) replication in HCV replicon systems[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HepG2 cells
Concentration: 1-25 µmol/L
Incubation Time: 24 h
Result: Induced mitochondrial uncoupling and AMPK activation not due to the non-specific cytotoxicity in HepG2 cells at concentrations less than 25 µmol/L.

Immunofluorescence[1]

Cell Line: HepG2 cells
Concentration: 10 µmol/L
Incubation Time: 24 h
Result: Promoted the nuclear translocation of TFEB by activating AMPK in HepG2 cells.

RT-PCR[1]

Cell Line: HepG2 cells
Concentration: 1-25 µmol/L
Incubation Time: 24 h
Result: Induced the increase transcription of SQSTM1/P62 in HepG2 cells.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 1-25 µmol/L
Incubation Time: 24 h
Result: Activated AMPK and increased phosphorylation of ACC in HepG2 cells.

Cell Cytotoxicity Assay[3]

Cell Line: RP7 cells, NTZ-11 and TIZ-9 cell lines
Concentration: The initial drug concentration was 0.02 µM, followed by 0.05, 0.1, 0.5, and 1 µM, and subsequent weekly increases of 1 µM until a final concentration of 11 µM.
Incubation Time: 3 days
Result: Againsted HCV replication in RP7 cells (IC50: 0.16), NTZ-11 (IC50:1.2) and TIZ-9 cell lines (IC50: 1.5)
In Vivo

Tizoxanide (TIZ) (10 mg/kg; i.v.) can pass the BBB and distribute to the brain tissue. Tizoxanide retains in brain is obviously longer than that in plasma[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague Dawley rats[2]
Dosage: 10 mg/kg
Administration: Tizoxanide (10 mg/kg; i.v.)
Result: Could pass the BBB and distribute to the brain tissue.
Molecular Weight

265.25

Formula

C10H7N3O4S

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(NC1=NC=C([N+]([O-])=O)S1)C2=CC=CC=C2O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (94.25 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : < 1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7700 mL 18.8501 mL 37.7003 mL
5 mM 0.7540 mL 3.7700 mL 7.5401 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  15% Cremophor EL    85% Saline

    Solubility: 5 mg/mL (18.85 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

  • Protocol 2

    Add each solvent one by one:  17% Solutol HS-15 in Saline

    Solubility: 5 mg/mL (18.85 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.09%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7700 mL 18.8501 mL 37.7003 mL 94.2507 mL
5 mM 0.7540 mL 3.7700 mL 7.5401 mL 18.8501 mL
10 mM 0.3770 mL 1.8850 mL 3.7700 mL 9.4251 mL
15 mM 0.2513 mL 1.2567 mL 2.5134 mL 6.2834 mL
20 mM 0.1885 mL 0.9425 mL 1.8850 mL 4.7125 mL
25 mM 0.1508 mL 0.7540 mL 1.5080 mL 3.7700 mL
30 mM 0.1257 mL 0.6283 mL 1.2567 mL 3.1417 mL
40 mM 0.0943 mL 0.4713 mL 0.9425 mL 2.3563 mL
50 mM 0.0754 mL 0.3770 mL 0.7540 mL 1.8850 mL
60 mM 0.0628 mL 0.3142 mL 0.6283 mL 1.5708 mL
80 mM 0.0471 mL 0.2356 mL 0.4713 mL 1.1781 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tizoxanide
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