Zanamivir - Influenza Virus 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEZanamivirCat. No.: HY-13210CAS No.: 139110-80-8分式: CHNO分量: 332.31作靶點(diǎn): Influenza Virus作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 33.33 mg/mL (100.30 mM)* means soluble

2、, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Zanamivir是流感病毒的神經(jīng)氨酸酶抑制劑，對(duì)于流感病毒A和B的IC50值分別為0.95 nM和2.7 nM。

3、IC50 & Target IC50: 0.95 nM (Influenza A); 2.7 nM (Influenza B) 1體外研究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 您邊的抑制劑師www.MedChemEsialic acid on the cell receptors, thus preventing release and spread of the newly formed virions 2.體內(nèi)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.戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) 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