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Baloxavir

CAS No. : 1985605-59-1

MCE 站：Baloxavir

产品活性：Baloxavir (Baloxavir acid)，衍生自前药 Baloxavir marboxil，是甲型和乙型流感病毒聚合酶 PA 亚基内的一种首创，有效且选择性的帽依赖性核酸内切酶 (CEN) 抑制剂。Baloxavir 抑制病毒 RNA 的转录和复制，并具有强大的抗病毒活性。

研究领域：Anti-infection

作用靶点：Influenza Virus

In Vitro: The median EC₅₀ values at baseline for Baloxavir (BXA) are 17.96 nM for A/H1N1pdm, 4.48 nM for A/H3N2, and 18.67 nM for type B virus.
Baloxavir (BXA) inhibits viral RNA transcription via selective inhibition of cap-dependent endonuclease (CEN) activity in enzymatic assays, and inhibits viral replication in infected cells without cytotoxicity in cytopathic effect assays. Baloxavir shows broad potency against various subtypes of influenza A viruses (H1N2, H5N1, H5N2, H5N6, H7N9 and H9N2). Additionally, serial passages of the viruses in the presence of Baloxavir result in isolation of PA/I38T variants with reduced BXA susceptibility.
Baloxavir (BXA) inhibits cap-dependent endonuclease (CEN) and CEN/RdRp activities with IC₅₀ values of 2.5 nM and 1.6 nM, respectively, while low potency (IC₅₀ >40 nM) is observed against RdRp activity.
Baloxavir (BXA) has a high inhibitory potency against CEN activity of the tested viral ribonucleoprotein complexes (vRNPs) from influenza A and B viruses with mean IC₅₀ values of 1.4-3.1 nM and 4.5-8.9 nM, respectively, indicating that Baloxavir has broad spectrum activities. Baloxavir shows high potency against influenza A and B viruses with mean EC₉₀ of 0.46 - 0.98 nM and 2.2-3.4 nM, respectively.

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