Maribavir-1263W94-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMaribavirCat. No.: HY-16305CAS No.: 176161-24-3Synonyms: 1263W94; BW1263W94; GW257406X分式: CHClNO分量: 376.24作靶點: CMV作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 51 mg/mL

2、 (135.55 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.6579 mL 13.2894 mL 26.5788 mL5 mM 0.5316 mL 2.6579 mL 5.3158 mL10 mM 0.2658 mL 1.3289 mL 2.6579 mL請根據(jù)產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Maribavir種有效抑制野型 pUL97 催化的組蛋磷酸

3、化，IC50 為 3 nM。Maribavir 可有效作于 HCMV和 Epstein-Barr 病毒 (EBV)。IC50 & Target HCMV 11/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Maribavir is a potent inhibitor of the autophosporylation of the wild type and all the major Ganciclovir (GCV)resistant UL97 mutants analysed with a mean IC50 of 35 nM.

4、 The M460I mutation results in hypersensitivityto Maribavir with an IC50 of 4.8 nM. A Maribavir resistant mutant of UL97 (L397R) is functionallycompromised as both a Ganciclovir kinase and a protein kinase ( 10% of wild type levels). Enzyme kineticexperiments demonstrate that Maribavir is a competit

5、ive inhibitor of ATP with a Ki of 10 nM 1. Maribavir(1263W94) inhibits viral replication in a dose-dependent manner, with IC50 of 0.120.01 M as measured bya multicycle DNA hybridization assay. The pUL97 protein kinase is strongly inhibited by Maribavir, with 50%inhibition occurring at 3 nM 2.PROTOCO

6、LKinase Assay 1 Enzyme kinetic analysis is performed on the purified wild type and mutant UL97 protein species usingincreasing concentrations of ATP (2 M to 20 M). The amount of incorporated radiolabelled phosphate isplotted against the concentration of ATP in a Lineweaver Burke plot to determine th

7、e Km for ATP for eachUL97 species. The effect of Maribavir upon the rate of radiolabelled phosphate incorporation by wild type ormutant UL97 is determined by protein kinase assays at a fixed concentration of Maribavir (0.5 M) as above,or with increasing concentrations of Maribavir (0.01 M to 5.0 M)

8、to determine the IC50 of Maribavir foreach UL97 species. In order to determine the nature of the inhibition mediated by Maribavir, plots of 1/v vs1/ATP with increasing concentrations of Maribavir are constructed. Competitive inhibition is evident if thefamily of lines cconverged on the y-axis at 1/V

9、max. The change in slope caused by the addition of Maribaviris used to calculate the Ki 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 For these studies MRC-5 cells are seeded in 24-well plates at 5104 cells/well and grown for 3 days inM

10、EM 8-1-1 to confluence (1.1105 cells/well). The cells are infected with AD169 in MEM 2-1-1 at an MOIranging from 1 to 3 and incubated at 37C for 90 min to allow viral adsorption. The unadsorbed virus isremoved and replaced with 1 mL of MEM 2-1-1. To test the effect of compounds on viral DNA synthesi

11、s ormaturation, Maribavir, BDCRB, or GCV is added to the medium at the concentrations indicated for eachexperiment 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發(fā)表的科研獻 J Biol Chem. 2019 Feb 19. pii: jbc.RA118.007049.See more customer validation

12、s on HYPERLINK / www.MedChemEREFERENCES1. Shannon-Lowe CD, et al. The effects of Maribavir on the autophosphorylation of ganciclovir resistant mutants of the cytomegalovirusUL97 protein. Herpesviridae. 2010 Dec 7;1(1):4.2. Biron KK, et al. Potent and selective inhibition of human cytomegalovirus replication by 1263W94, a benzimidazole L-riboside with a2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEunique mode of action. Antimicrob Agents Chemother. 2002 Aug;46(8):2365-72.McePdfHeightC