| Description | Baloxavir (S-033447) is a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit. |
| In vitro | Baloxavir (BXA) 通过选择性地抑制帽依赖性内切酶 (CEN) 活性来抑制病毒RNA转录，并在细胞病理效应试验中抑制被感染细胞中的病毒复制而不产生细胞毒性。此外，Baloxavir 对帽依赖性内切酶 (CEN) 和 CEN/RdRp 活性显示出高抑制性，IC50 值分别为 2.5 nM 和 1.6 nM，而对 RdRp 活性的抑制力低 (IC50 >40 nM)。Baloxavir 在基线时对 A/H1N1pdm、A/H3N2 和 B型病毒的中位 EC50 值分别为 17.96 nM、4.48 nM 和 18.67 nM。针对流感A型和B型病毒，Baloxavir 表现出高效力，EC90 平均值分别为 0.46 - 0.98 nM 和 2.2-3.4 nM，且对各种亚型的流感A型病毒 (H1N2、H5N1、H5N2、H5N6、H7N9 和 H9N2) 也显示广泛的效力。连续通过含 Baloxavir 的病毒系列使得 PA/I38T 变异体与减少的 BXA 敏感性出现。Baloxavir 对于测试的流感A型和B型病毒的病毒核糖核蛋白复合体 (vRNPs) 的 CEN 活性具有高抑制效力，平均 IC50 值分别为 1.4-3.1 nM 和 4.5-8.9 nM，表明 Baloxavir 具有广谱活性。 |
| Synonyms | Baloxavir acid, S-033447 |
| molecular weight | 483.49 |
| Molecular formula | C24H19F2N3O4S |
| CAS | 1985605-59-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (93.07 mM) |
| References | 1. Omoto S, et al. Characterization of influenza virus variants induced by treatment with the endonuclease inhibitor baloxavir marboxil. Sci Rep. 2018 Jun 25;8(1):9633. 2. Noshi T, et al. In vitro characterization of baloxavir acid, a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit. Antiviral Res. 2018 Dec;160:109-117. |
| Citations | 1. Liu K, Li L, Liu Y, et al.Discovery of baloxavir sodium as a novel anti-CCHFV inhibitor: biological evaluation of in vitro and in vivo.Antiviral Research.2024: 105890. |