Baloxavir

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Chemical Structure| 1985605-59-1 同义名 : -
CAS号 : 1985605-59-1
货号 : A1145224
分子式 : C24H19F2N3O4S
纯度 : 97%
分子量 : 483.49
MDL号 : MFCD31619273
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(82.73 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Baloxavir, derived from the prodrug Baloxavir marboxil, is a potent, selective cap-dependent endonuclease (CEN) inhibitor of the PA subunit of influenza A and B viral polymerase, a first-in-class inhibitor of viral RNA transcription and replication, and possesses potent antiviral activity. Baloxavir inhibits both cap-dependent endonuclease (CEN) and cap-dependent endonuclease (CEN). Baloxavir inhibits cap-dependent endonuclease (CEN) and CEN/RdRp activity with IC50 values of 2.5 nM and 1.6 nM, respectively, while the inhibitory efficacy against RdRp activity is low (IC50 >40 nM)[1][2].The median EC50 values of Baloxavir against A/H1N1pdm, A/H3N2 and B viruses were 17.96 nM, 4.48 nM and 18.67 nM, respectively[1].Baloxavir inhibits viral RNA transcription by inhibiting cap-dependent endonuclease (CEN) activity, and inhibits viral replication in infected cells without cytotoxicity in cytopathic effect assays. Baloxavir has a broad spectrum of efficacy against various subtypes of influenza A viruses (H1N2, H5N1, H5N2, H5N6, H7N9 and H9N2). In addition, sequential passaging of the viruses in the presence of Baloxavir resulted in the isolation of PA/I38T variants with reduced susceptibility to BXA. Baloxavir showed high potency to inhibit CEN activity in the tested influenza A and B virus ribonucleoprotein complexes (vRNPs), with mean IC50 values of 1.4-3.1 nM and 4.5-8.9 nM, respectively, indicating broad-spectrum activity. Baloxavir was highly potent against influenza A and B viruses, with mean EC90 values of 0.46-0.98 nM and 2.2-3.4 nM, respectively[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.34mL

2.07mL

1.03mL

20.68mL

4.14mL

2.07mL
参考文献

[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.