Home Microbiology Antiviral inhibitor Baloxavir marboxil

Baloxavir marboxil

Catalog No.S5952

For research use only.

Baloxavir marboxil, a cap-endonuclease inhibitor, is an antiviral drug.

Baloxavir marboxil Chemical Structure

CAS No. 1985606-14-1

Selleck's Baloxavir marboxil has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description Baloxavir marboxil, a cap-endonuclease inhibitor, is an antiviral drug.
In vivo

Single-dose oral baloxavir marboxil is well tolerated, had a favorable safety profile, and has favorable pharmacokinetic characteristics, including a long half-life, supporting single oral dosing. In nonclinical studies, baloxavir marboxil is a prodrug and is converted to an active form, baloxavir acid, by hydrolysis. After single oral administration in rats and monkeys, plasma concentrations of baloxavir marboxil are below the lower limit of quantification (LLOQ) at all sampling points, and area under the plasma concentration-time curve of baloxavir acid increased dose proportionally. The major excretion route of radioactivity is via fecal excretion, whereas urinary excretion was low in rats and monkeys[3]. Baloxavir marboxil has shown therapeutic activity in preclinical models of influenza A and B virus infections, including strains resistant to current antiviral agents. In murine models of seasonal influenza and avian influenza A(H5N1) or A(H7N9), orally administered baloxavir is associated with rapid reductions in pulmonary viral loads and decreased mortality[1].

Protocol (from reference)

Animal Research:

[2]
  • Animal Models: Specific-pathogen-free, 6-week-old BALB/c mice
  • Dosages: 0.5, 1.5, 15 or 50 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 571.55
Formula

C27H23F2N3O7S
CAS No. 1985606-14-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC(=O)OCOC1=C2C(=O)N3CCOCC3N(N2C=CC1=O)C4C5=C(CSC6=CC=CC=C46)C(=C(C=C5)F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03653364 Recruiting Drug: Baloxavir Marboxil Influenza Hoffmann-La Roche January 23 2019 Phase 3
NCT03629184 Completed Drug: Baloxavir Marboxil|Drug: Oseltamivir Influenza Hoffmann-La Roche November 20 2018 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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