HIV-1; HBV/HCV (EC50 = 0.46μM and 0.15 μM)

体外活性：Tizoxanide 是 Nitazoxanide 的活性代谢物，Nitazoxanide 是一种噻唑类抗感染化合物，可对抗厌氧菌、原生动物和一系列病毒。 IC50值：目标：体外抗病毒剂：替佐尼特抑制所有CIV的病毒复制，抑制浓度分别为0.17至0.21μM和0.60至0.76μM，抑制浓度为50％和90％。硝唑尼特及其主要代谢物替唑尼特可抑制丙型肝炎病毒 (HCV) 复制子系统中的复制。有趣的是，硝唑尼特或替唑尼特的连续传代导致对α干扰素2b的敏感性增加：EC(50)s和EC(90)s分别降低三倍和八倍。激酶测定： 细胞测定：

硝唑尼特以 250 mg/kg/天的剂量口服给药 11 天，可部分有效减少限生仔猪腹泻模型中的寄生虫负担，但 125 mg/kg/天的剂量则无效。硝唑尼特会引起仔猪药物相关性腹泻，这可能会影响其治疗效果。

Metabolism / Metabolites
Tizoxanide has known human metabolites that include (2S,3S,4S,5R)-3,4,5-Trihydroxy-6-[2-[(5-nitro-1,3-thiazol-2-yl)carbamoyl]phenoxy]oxane-2-carboxylic acid.

[1]. Antimicrob Agents Chemother.1998 Aug;42(8):1959-65.

[2]. Clin Infect Dis.2005 Apr 15;40(8):1173-80.

Desacetyl-nitazoxanide is a member of salicylamides.

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Nitazoxanide (NTZ), a drug currently being tested in human clinical trials for efficacy against chronic cryptosporidiosis, was assessed in cell culture and in two animal models. The inhibitory activity of NTZ was compared with that of paromomycin (PRM), a drug that is partially effective against Cryptosporidium parvum. A concentration of 10 microg of NTZ/ml (32 microM) consistently reduced parasite growth in cell culture by more than 90% with little evidence of drug-associated cytotoxicity, in contrast to an 80% reduction produced by PRM at 2,000 microg/ml (3.2 mM). In contrast to its efficacy in vitro, NTZ at either 100 or 200 mg/kg of body weight/day for 10 days was ineffective at reducing the parasite burden in C. parvum-infected, anti-gamma-interferon-conditioned SCID mice. Combined treatment with NTZ and PRM was no more effective than treatment with PRM alone. Finally, NTZ was partially effective at reducing the parasite burden in a gnotobiotic piglet diarrhea model when given orally for 11 days at 250 mg/kg/day but not at 125 mg/kg/day. However, the higher dose of NTZ induced a drug-related diarrhea in piglets that might have influenced its therapeutic efficacy. As we have previously reported, PRM was effective at markedly reducing the parasite burden in piglets at a dosage of 500 mg/kg/day. Our results indicate that of all of the models tested, the piglet diarrhea model most closely mimics the partial response to NTZ treatment reported to occur in patients with chronic cryptosporidiosis. [1]

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Nitazoxanide is a new thiazolide antiparasitic agent that shows excellent in vitro activity against a wide variety of protozoa and helminths. It is given by the oral route with good bioavailability and is well tolerated, with primarily mild gastrointestinal side effects. At present, there are no documented drug-drug interactions. Nitazoxanide has been licensed for the treatment of Giardia intestinalis-induced diarrhea in patients >or=1 year of age and Cryptosporidum-induced diarrhea in children aged 1-11 years. At present, it is pending licensure for treatment of infection due to Cryptosporidium species in adults and for use in treating immunocompromised hosts. It represents an important addition to the antiparasitic arsenal. [2]

C10H7N3O4S

265.25

265.015

C, 45.28; H, 2.66; N, 15.84; O, 24.13; S, 12.09

173903-47-4

Tizoxanide-d4;1246817-56-0

394397

Solid powder

1.6±0.1 g/cm3

279-281ºC(dec)

1.750

2.91

136.28

2

6

2

18

336

0

S1C(=C([H])N=C1N([H])C(C1=C([H])C([H])=C([H])C([H])=C1O[H])=O)[N+](=O)[O-]

FDTZUTSGGSRHQF-UHFFFAOYSA-N

InChI=1S/C10H7N3O4S/c14-7-4-2-1-3-6(7)9(15)12-10-11-5-8(18-10)13(16)17/h1-5,14H,(H,11,12,15)

2-hydroxy-N-(5-nitrothiazol-2-yl)benzamide

NSC-697856; NSC697856; Tizoxanide; 173903-47-4; 2-hydroxy-N-(5-nitrothiazol-2-yl)benzamide; Benzamide, 2-hydroxy-N-(5-nitro-2-thiazolyl)-; Desacetyl-nitazoxanide; NSC-697856; 2-hydroxy-N-(5-nitro-1,3-thiazol-2-yl)benzamide; UNII-15KFG88UOJ; NSC697856; Tizoxanide; Desacetylnitazoxanide; Desacetyl-nitazoxanide;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~25 mg/mL (~94.25 mM)
Ethanol : < 1 mg/mL

配方 1 中的溶解度: 5 mg/mL (18.85 mM) in 15% Cremophor EL + 85% Saline (这些助溶剂从左到右依次添加，逐一添加), 悬浮液； 超声助溶 (<60°C).
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: 15% Cremophor EL+85% Saline: 5 mg/mL (18.85 mM)

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配方 3 中的溶解度: 5 mg/mL (18.85 mM) in 17% Polyethylene glycol 12-hydroxystearate in Saline (这些助溶剂从左到右依次添加，逐一添加), 悬浮液； 超声助溶 (<60°C).
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。