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。

Baloxavir (Baloxavir acid), derived from the prodrug Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity.

Solid

Influenza virus Cap-dependent endonuclease (CEN)

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.

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[1]. Omoto S, et al. Characterization of influenza virus variants induced by treatment with the endonuclease inhibitor baloxavir marboxil. Sci Rep. 2018 Jun 25;8(1):9633.
[2]. Noshi T, et al. In vitro characterization of baloxavir acid, a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit. Antiviral Res. 2018 Dec;160:109-117.

In Vitro: DMSO : 41.67 mg/mL (86.19 mM; Need ultrasonic)配制储备液