Maribavir ≥98%
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| 包装规格: | 5mg 25mg 100mg in glass bottle |
| 溶解性: | 溶于DMSO(200 mg/mL 超声) |
| 产品描述: | 基本信息 产品编号:M10644 产品名称:Maribavir CAS: 176161-24-3 储存条件 粉末 -20℃ 四年 分子式: C15H19Cl2N3O4 溶于液体 -80℃ 两年 分子量 376.24 -20℃ 一个月 化学名: (2S,3S,4R,5S)-2-(5,6-dichloro-2-(isopropylamino)-1H-benzo[d]imidazol-1-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol Solubility (25°C) 体外 DMSO 200mg/mL (531.58mM Need ultrasonic) Ethanol Water 体内 现配现用 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 2.6579mL 13.2894mL 26.5788mL 5mM 0.5316mL 2.6579mL 5.3158mL 10mM 0.2658mL 1.3289mL 2.6579mL 生物活性 产品描述 一种有效抑制野生型 pUL97 催化的组蛋白磷酸化,IC50 为 3 nM。 靶点/IC50 HCMV 体外研究 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 35nM. The M460I mutation results in hypersensitivity to Maribavir with an IC50 of 4.8nM. A Maribavir resistant mutant of UL97 (L397R) is functionally compromised as both a Ganciclovir kinase and a protein kinase (~ 10% of wild type levels). Enzyme kinetic experiments demonstrate that Maribavir is a competitive inhibitor of ATP with a Ki of 10nM. Maribavir (1263W94) inhibits viral replication in a dose-dependent manner, with IC50 of 0.12±0.01μM as measured by a multicycle DNA hybridization assay. The pUL97 protein kinase is strongly inhibited by Maribavir, with 50% inhibition occurring at 3nM. 推荐实验方法(仅供参考) 激酶实验: Kinase Assay Enzyme kinetic analysis is performed on the purified wild type and mutant UL97 protein species using increasing concentrations of ATP (2μM to 20μM). The amount of incorporated radiolabelled phosphate is plotted against the concentration of ATP in a Lineweaver Burke plot to determine the Km for ATP for each UL97 species. The effect of Maribavir upon the rate of radiolabelled phosphate incorporation by wild type or mutant UL97 is determined by protein kinase assays at a fixed concentration of Maribavir (0.5μM) as above, or with increasing concentrations of Maribavir (0.01μM to 5.0μM) to determine the IC50 of Maribavir for each UL97 species. In order to determine the nature of the inhibition mediated by Maribavir, plots of 1/v vs 1/ATP with increasing concentrations of Maribavir are constructed. Competitive inhibition is evident if the family of lines cconverged on the y-axis at 1/Vmax. The change in slope caused by the addition of Maribavir is used to calculate the Ki 细胞实验: Cell Assay For these studies MRC-5 cells are seeded in 24-well plates at ~5×104 cells/well and grown for 3 days in MEM 8-1-1 to confluence (~1.1×105 cells/well). The cells are infected with AD169 in MEM 2-1-1 at an MOI ranging from 1 to 3 and incubated at 37°C for 90min to allow viral adsorption. The unadsorbed virus is removed and replaced with 1mL of MEM 2-1-1. To test the effect of compounds on viral DNA synthesis or maturation, Maribavir, BDCRB, or GCV is added to the medium at the concentrations indicated for each experiment. |
| 保存条件: | -20℃ |
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