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抑制剂描述:

产品名称:Nitazoxanide

产品别名:见爱必信官网

英文别名:Nitazoxanide

靶点:Antiparasitic

CAS:55981-09-4

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Nitazoxanide (Alinia, Annita) is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent. (IC50 for canine influenza virus ranges from 0.17 to 0.21 μM) The anti- protozoal activity of nitazoxanide is believed to be due to interference with the pyruvate:ferredoxin oxidoreductase (PFOR) enzyme dependent electron transfer reaction which is essential to anaerobic energy metabolism. It has also been shown to have activity against influenza A virus. Nitazoxanide and tizoxanide inhibited virus replication of all canine influenza virus with 50% and 90% inhibitory concentrations ranging from 0.17 to 0.21 μM and from 0.60 to 0.76 μM, respectively.

溶解性:DMSO :58 mg/mL (188.8 mM)

体外研究:

Nitazoxanide reduces parasite growth in cell culture by more than 90% with little evidence of drug-associated cytotoxicity. Nitazoxanide is a new thiazolide antiparasitic agent that shows excellent in vitro activity against a wide variety of protozoa and helminths. Nitazoxanide and its metabolite tizoxanide are more active in vitro than metronidazole against G. intestinalis, E. histolytica and T. vaginalis. Nitazoxanide exhibits potent inhibition of both HBV and HCV replication. Nitazoxanide potentiates the effect of subsequent treatment with Nitazoxanide plus IFN, but not Nitazoxanide plus 2'CmeC, in HCV replicon-containing cells. Nitazoxanide induces reductions in several HBV proteins (HBsAg, HBeAg, HBcAg) produced by 2.2.15 cells, but does not affect HBV RNA transcription. Nitazoxanide exhibits IC50, and IC90 values of 0.017 and 0.776 mg/mL respectively, against E. histolytica, 0.004 and 0.067 mg/mL against G. intestinalis, and 0.034 and 2.046 mg/mL against T. vaginalis. Nitazoxanide is more toxic than metronidazole and albendazole against E. histolytica.

体内研究:Nitazoxanide is 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. Nitazoxanide induces a drug-related diarrhea in piglets that might have influenced its therapeutic efficacy.

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