| Name | Baloxavir |
| Description | Baloxavir (S-033447) is a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit. |
| 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[2]. 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[1]. 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[2] 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[2]. 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 46 mg/mL (95.14 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.14 mM), Sonication is recommended.
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| Keywords | transcription | S033447 | S 033447 | RNA | InfluenzaVirus | Influenza virus | influenza | endonuclease | dolutegravir | CEN | cap-dependent | BXA | Baloxavir |
| Inhibitors Related | Rifampicin | Acetylcysteine | α-Vitamin E | Molnupiravir | Nitazoxanide | Curcumin | Naringenin | Salcomine | Benzimidazole | Dihydromyricetin | β-Cyclodextrin | Crystal Violet |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | ReFRAME Related Library | Drug-induced Liver Injury (DILI) Compound Library | Toxic Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Infection Compound Library | Human Metabolite Library |
United States
