gs 441524

GS-441524 是 Remdesivir 的主要活性代谢物，活性更优于 Remdesivir ，治疗患有自然发生的猫传染性腹膜炎的猫。

GS-441524tris-isobutyryl ester is a prodrug form of the antiviral nucleoside analog and remdesivir metabolite GS-441524 .1It reduces the cytopathic effect of respiratory syncytial virus (RSV) in infected HEp-2 cells with an EC50value of 0.26 μM. 1.Mackman, R.L., Hui, H.C., Perron, M., et al.Prodrugs of a 1’-CN-4-aza-7,9-dideazaadenosine C-nucleoside leading to the discovery of remdesivir (GS-5734) as a potent inhibitor of respiratory syncytial virus with efficacy in the african green monkey model of RSVJ. Med. Chem.64(8)5001-5017(2021)

E197 是一种抗骨质疏松化合物，是一种 Dock5 抑制剂，可用于研究骨质疏松。

GS-441524 is a potent inhibitor of feline infectious peritonitis (FIP) virus with an EC50 of 0.78 μM.. GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies. GS-441524 is a molecular precursor to a pharmacologically active nucleoside triphosphate molecule. These analogs act as an alternative substrate and RNA-chain terminator of viral RNA dependent RNA polymerase. GS-441524 was non-toxic in feline cells at concentrations as high as 100 uM and effectively inhibited FIPV replication in cultured CRFK cells and in naturally infected feline peritoneal macrophages at concentrations as low as 1 uM. Note: GS-441524 is an active metabolite of Remdesivir.

Remdesivir triphosphate 是一种有效的病毒 RNA 依赖的 RNA 聚合酶抑制剂，对RSVRdRp 和 HCVRdRp 的IC50分别为 1.1 µM 和 5 µM。它是 Remdesivir 的活性三磷酸代谢物。

GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC 50 s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734).

GS-621763 是具有口服活性的 GS-441524 前药，在小鼠体内具有抗SARS-CoV-2病毒活性。

SHEN26 (ATY014) 是一种有效且具有口服活性的 RdRp 抑制剂，对 SARS-CoV-2 的 IC50 为 1.36 μM。SHEN26 是 GS-441524 的 5’-环己烷甲酸酯衍生物，通过抑制病毒核酸合成达到抗病毒作用，可用于冠状病毒2019 (COVID-19) 的研究。