| Description | Bemnifosbuvir (AT-511) is a novel phosphoramidate prodrug of 2'-fluoro-2'-C-methylguanosine-5'-monophosphate that has potent in vitro activity against HCV. |
| In vitro | Bemnifosbuvir是一种新型的2'-氟-2'-C-甲基鸟苷-5'-一磷酸盐前体化合物，对HCV[1]具有强大的体外活性。在无细胞的情况下，Bemnifosbuvir在37°C的培养基中孵育24小时仍保持稳定。在所有肝细胞种类以及Huh-7细胞中，用10μM Bemnifosbuvir孵育后，AT-9010是测定的主要细胞内代谢产物；除鼠肝细胞外，其浓度远高于细胞内Bemnifosbuvir浓度，表明从其磷酰胺前药中有效生成活性三磷酸（TP）。在肝细胞孵育中，形成AT-9010的相对水平及其在24小时内的积累（以曲线下面积或AUC0-24h表示），从多到少依次为大鼠>人类>小鼠>狗/猴。 |
| In vivo | 经每8小时一次的moxifloxacin治疗的动物存活时间较其他所有组别更长。细菌挑战30小时后的组织培养结果显示，moxifloxacin处理的动物的脾脏和肺部的细菌生长明显少于其他组别，但其肝脏中的细菌生长情况并无显著差异[2]。 |
| Target activity | HCV:5-28 nM (EC50), SARS-CoV-2:0.47 μM (EC90) |
| Synonyms | AT-511 |
| molecular weight | 581.53 |
| Molecular formula | C24H33FN7O7P |
| CAS | 1998705-64-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 95 mg/mL (163.36 mM) |
| References | 1. Steven S Good, et al. Preclinical evaluation of AT-527, a novel guanosine nucleotide prodrug with potent, pan-genotypic activity against hepatitis C virus. PLoS One. 2020 Jan 8;15(1):e0227104. 2. Ioannidis O, et al. Effect of moxifloxacin on survival, lipid peroxidation and inflammation in immunosuppressed rats with soft tissue infection caused by Stenotrophomonas maltophilia. Microbiol Immunol. 2014 Feb;58(2):96-102. |