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Baloxavir

SKU: orb1308587

Description

Baloxavir (S-033447) is a novel small-molecule inhibitor that selectively targets the PA subunit of the influenza virus polymerase, acting via cap-dependent endonuclease inhibition. It is widely used in antiviral research for both in vitro mechanistic studies and in vivo efficacy models, supporting the development of novel anti-influenza therapeutics.

Research Area

Infectious Disease & Virology

Images & Validation

Key Properties

CAS Number1985605-59-1
MW483.49
Purity99.46%
FormulaC24H19F2N3O4S
SMILESOc1c2C(=O)N3CCOC[C@H]3N([C@@H]3c4ccccc4SCc4c(F)c(F)ccc34)n2ccc1=O
TargetInfluenza Virus
SolubilityDMSO:46 mg/mL (95.14 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.14 mM)

Bioactivity

In Vitro
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, and it also 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. 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 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 and it also 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) 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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

dolutegravir, CEN, Baloxavir, Baloxavir acid, BXA, cap-dependent, InfluenzaVirus, Influenza Virus, Influenza virus, influenza, endonuclease, RNA, S 033447, S033447, S-033447, transcription

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Key Properties

No computed properties available.

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Baloxavir (orb1308587)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 120.00
5 mg
$ 220.00
1 ml x 10 mM (in DMSO)
$ 230.00
10 mg
$ 320.00
25 mg
$ 570.00
50 mg
$ 720.00
100 mg
$ 1,000.00
200 mg
$ 1,330.00
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