| Description | Galidesivir (BCX4430) is a broad-spectrum antiviral compound, an adenosine analog that inhibits viral RNA-dependent RNA polymerase (RdRp) activity.Galidesivir inhibits a wide range of RNA viral pathogens in vitro, and reduces lung infections in infected animals. |
| In vitro | Galidesivir (BCX4430) 在细胞激酶的作用下磷酸化形成三磷酸。Galidesivir 的单磷酸核苷酸被病毒RNA聚合酶合成到增长中的RNA链中，导致提前终止链延伸[1]。在抑制黄热病毒（YFV）感染Vero细胞的过程中，Galidesivir显示出有效性。Galidesivir 在中性红素摄取试验中的EC50值为8.3 μg/ml (24.5 μM)[4]。 |
| In vivo | Galidesivir（BCX4430）在多种实验感染模型中通过肌肉注射、腹腔注射和口服途径展现了活性。非临床研究表明，Galidesivir对致命的埃博拉病毒、马尔堡病毒、裂谷热病毒和黄热病病毒感染具有显著疗效[1]。在黄热（YF）仓鼠模型中每天两次通过腹腔注射4 mg/kg7天，Galidesivir显示出有效性[3]。 |
| Target activity | neutral red uptake assay:24.5 μM (EC50) |
| Synonyms | BCX4430, Immucillin-A |
| molecular weight | 265.27 |
| Molecular formula | C11H15N5O3 |
| CAS | 249503-25-1 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | H2O: 50 mg/mL (188.49 mM), Sonication is recommended. |
| References | 1. Taylor R, et al. BCX4430 - A broad-spectrum antiviral adenosine nucleoside analog under development for the treatment of Ebola virus disease. J Infect Public Health. 2016;9(3):220-226. 2. Elfiky AA, et al. ICN-1229, Remdesivir, PSI-7977, Galidesivir, and GS 1278 against SARS-CoV-2 RNA dependent RNA polymerase (RdRp): A molecular docking study. Life Sci. 2020 Mar 25:117592. 3. Julander JG, et al. BCX4430, a novel nucleoside analog, effectively treats yellow fever in a Hamster model. Antimicrob Agents Chemother. 2014;58(11):6607-6614. 4. Warren TK, et al. Protection against filovirus diseases by a novel broad-spectrum nucleoside analogue BCX4430. Nature. 2014;508(7496):402-405. |