Nitazoxanide (NTZ) 是一种广谱驱虫剂 (anthelmintic)，对感染动物和人类的各种蠕虫、原生动物和肠道细菌都具有作用活性。 Nitazoxanide 在无菌培养中抑制Giardia lamblia滋养体增殖，IC50为 2.4 μM。Nitazoxanide 可用于寄生虫性 (parasitic) 胃肠炎的研究。Nitazoxanide还具有抗病毒特性。 Nitazoxanide 在小鼠模型中显示出抗日本脑炎病毒 (JEV) 活性。
| 生物活性 | Nitazoxanide (NTZ), ananthelminticagent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infectinganimalsand humans. Nitazoxanide inhibitsGiardia lambliatrophozoite proliferation in axenic culture with an IC50of 2.4 μM[1]. Nitazoxanide can be used for the research ofparasiticgastroenteritis. Nitazoxanide shows anti-Japanese encephalitis virus (JEV) activity in a mouse model[2]. |
体外研究
(In Vitro) | Giardia lamblia, a flagellated protozoan, is the most common causative agent of persistent diarrhea worldwide[1].
Nitazoxanide exhibits effect onG. lambliatrophozoite proliferation in axenic culture with an IC50of 2.4 μM[1].
Cell Viability Assay[1] | Cell Line: | Human cancer colon Caco2 cells were incubated with increasing numbers of Giardia lamblia trophozoites (103to 106parasites 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 105parasites 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 105trophozoites. |
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体内研究
(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[1].
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[2].
| Animal Model: | Three-week old female Chinese Kunming mice (12–14 g body weight) were infected intraperitoneally with JEV[2] | | 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. |
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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 : ≥ 100 mg/mL(325.44 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.2544 mL | 16.2718 mL | 32.5436 mL | | 5 mM | 0.6509 mL | 3.2544 mL | 6.5087 mL | | 10 mM | 0.3254 mL | 1.6272 mL | 3.2544 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 3.25 mg/mL (10.58 mM); Clear solution
此方案可获得 ≥ 3.25 mg/mL (10.58 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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