| Description | Maribavir (GW257406X) is an orally available benzimidazole riboside compound with activity against cytomegalovirus (CMV). Maribavir is a selective ATP competitor of the viral UL97 kinase, which is involved in viral nuclear maturation events, such as viral DNA assembly and movement of viral capsids from the nucleus of infected cells. Maribavir has activity against strains of CMV that are resistant to standard anti-CMV agents. |
| In vitro | Maribavir是一种强效的抑制剂，能够有效抑制野生型及所有主要的Ganciclovir（GCV）耐药UL97突变体的自磷酸化，平均IC50值为35 nM。M460I突变体对Maribavir表现出超敏感性，IC50值为4.8 nM。Maribavir耐药的UL97突变体（L397R）在功能上受到损害，无论作为Ganciclovir激酶还是蛋白激酶的表现都大大降低（约为野生型的10%）。酶动力学实验表明，Maribavir是ATP的竞争性抑制剂，Ki值为10 nM[1]。Maribavir（1263W94）能够以剂量依赖的方式抑制病毒复制，通过多周期DNA杂交分析测得的IC50为0.12±0.01 μM。pUL97蛋白激酶被Maribavir强烈抑制，50%抑制浓度为3 nM[2]。 |
| Cell experiments | Maribavir (1263W94) is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. 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 90 min to allow viral adsorption. The unadsorbed virus is removed and replaced with 1 mL 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[2]. |
| Target activity | Histone phosphorylation:3 nM |
| Synonyms | BW1263W94, GW257406X, Benzimidavir, 马立巴韦, 1263W94 |
| molecular weight | 376.24 |
| Molecular formula | C15H19Cl2N3O4 |
| CAS | 176161-24-3 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (159.47 mM) |
| References | 1. Shannon-Lowe CD, et al. The effects of Maribavir on the autophosphorylation of ganciclovir resistant mutants of the cytomegalovirus UL97 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 a unique mode of action. Antimicrob Agents Chemother. 2002 Aug;46(8):2365-72. |