Tizoxanide (TIZ) 是 Nitazoxanidede 的活性代谢物，也是一种噻唑胺类抗感染化合物，对厌氧菌、原生动物和一系列病毒产生作用。Tizoxanide (TIZ) 具有抗HIV-1活性，对 HBV 和 HCV 的复制有较强的抑制作用，EC50 分别为 0.46 μM 和 0.15 μM。Tizoxanide (TIZ) 还通过抑制 LPS 处理的巨噬细胞中促炎细胞因子的产生和 NF-κB 以及 MAPK 信号通路的激活发挥抗炎作用。
| 生物活性 | Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolideanti-infectivecompound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) hasanti-HIV-1activities and potent inhibition of bothHBVandHCVreplication with valuesEC50of 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 theNF-κBand the MAPK signaling pathways in LPS-treated macrophage cells[1][3][4][5]. |
| IC50& Target | Tizoxanide (TIZ) has potent inhibition of both HBV and HCV replication with valuesEC50of 0.46μM and 0.15 μM, respectively[4]. |
体外研究
(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].
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) |
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体内研究
(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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 38 mg/mL(143.26 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.7700 mL | 18.8501 mL | 37.7003 mL | | 5 mM | 0.7540 mL | 3.7700 mL | 7.5401 mL | | 10 mM | 0.3770 mL | 1.8850 mL | 3.7700 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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