Zanamivir - Influenza Virus 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEZanamivirCat. No.: HY-13210CAS No.: 139110-80-8分式: CHNO分量: 332.31作靶点: Influenza Virus作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 33.33 mg/mL (100.30 mM)* means soluble

2、, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.0092 mL 15.0462 mL 30.0924 mL5 mM 0.6018 mL 3.0092 mL 6.0185 mL10 mM 0.3009 mL 1.5046 mL 3.0092 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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Zanamivir是流感病毒的神经氨酸酶抑制剂，对于流感病毒A和B的IC50值分别为0.95 nM和2.7 nM。

3、IC50 & Target IC50: 0.95 nM (Influenza A); 2.7 nM (Influenza B) 1体外研究Zanamivir interacts with a group of amino acids in the active site of neuraminidase, which are conserved inall influenza A and B strains. Zanamivir blocks the action of neuraminidase, which prevents the cleavage of1/2 Master of Sma

4、ll Molecules 您边的抑制剂师www.MedChemEsialic acid on the cell receptors, thus preventing release and spread of the newly formed virions 2.体内研究 Zanamivir has a poor bioavailability in oral administration, with only 417% of the agent. Oral delivery ofzanamivir has been a problem due to its strong hydrophili

5、c nature that limits its transport across the intestinalepithelium. Permeation enhancers such as sodium cholate, hydroxypropyl -cyclodextrin could be used withzanamivir to enhance the intestinal permeability 3.PROTOCOLAnimal Rats: Formulations PO-SC (Zanamivir with SC for p.o.) and PO-C (Zanamivir c

6、ontrol solution for p.o.) areAdministration 3 administered orally at a Zanamivir dose of 10 mg/kg, and IV-R (reference Zanamivir saline solution for i.v.) isadministered i.v. at a dose of 1 mg/kg to rats under conscious condition. Blood samples are collected prior toand at 0.5, 1, 2, 3, 4, 6, 8, and

7、 24 hr after administration. At each sampling point, three rats from each groupare sacrificed after blood collection to extract the lungs. The lungs are cleansed with saline after extraction oflungs from the rats through a chest incision. The lungs are then transferred into E-tube and stored in thef

8、reezer (-80C) until analysis. Plasma samples are harvested by centrifugation at 1,500 g for 10 min andstored at -20C until analysis. The analysis of Zanamivir in both plasma and lungs is performed using before-mentioned LC-MS/MS method 3.MCE has not independently confirmed the accuracy of these meth

9、ods. They are for reference only.户使本产品发表的科研献 PLoS One. 2018 Jul 12;13(7):e0200761. bioRxiv. July 26, 2018.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Gubareva LV, et al. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates ofinflu

10、enza virusand neuraminidase inhibitor-resistant variants. Antimicrob Agents Chemother. 2001 Dec;45(12):3403-8.2. McKimm-Breschkin JL, et al. Management of influenza virus infections with neuraminidase inhibitors: detection, incidence, andimplications of drug resistance. Treat Respir Med. 2005;4(2):107-16.3. Shanmugam S, et al. Zanamivir oral delivery: enhanced plasma and lung bioavailability in rats. Biomol Ther (Seoul). 2013Mar;21(2):161-9.McePdfHeightCaution: Product has not been ful