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GS-441524

CAS No. : 1191237-69-0

MCE 站：GS-441524

产品活性：GS-441524 是 Remdesivir 的主要活性代谢物，活性更优于 Remdesivir ，感染病毒的原代人肺和猫细胞的细胞模型中显示出相似的活性。 GS-441524 对猫传染性腹膜炎病毒 (FIPV) 有较强的抑制作用，对应的 EC₅₀ 值为 0.78 μM。

研究领域：Cell Cycle/DNA Damage  |  Anti-infection

作用靶点：DNA/RNA Synthesis  |  SARS-CoV

In Vitro: The cells appear ａnd grow normally at all concentrations of GS-441524 ａnd fail to uptake the fluorescent dye CellTox Green at 24 h. The cytotoxic concentration-50% (CC50) is therefore>100 μM. The effective concentration-50% (EC₅₀) of GS-441524 is calculated to be 0.78 μM.

In Vivo: All 10 treated cats have a rapid response to treatment ａnd lymphocyte levels ａnd rectal temperatures return to pre-infection levels ａnd levels of the two asymptomatic cats. All ten of the once or twice treated cats have remained normal to date (more than eight months post infection). Injections cause a transient "stinging" reaction in some cats within 10 s of compound administration. Localized ａnd transient pain is evidenced by unusual posturing, licking at the injection site and/or vocalizations that last for approximately 30-60 s after injection. Injection reactions are more pronounced in some animals relative to others ａnd reactions are inconsistent from one injection to the next ａnd decreas over time.
Remdesivi (IV injection) in NHP results in GS-441524 being present in serum at concentrations 1000-fold higher than Remdesivir throughout a 7-day treatment course.

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