Baloxavir marboxil

Synonyms: S-033188

Baloxavir marboxil(S-033188), a cap-endonuclease inhibitor, is an antiviral drug.

Baloxavir marboxil Chemical Structure

Baloxavir marboxil Chemical Structure

CAS No. 1985606-14-1

Purity & Quality Control

Batch: S595201 DMSO]100 mg/mL]false]Ethanol]7 mg/mL]false]Water]Insoluble]false Purity: 99.92%
99.92

Baloxavir marboxil Related Products

Biological Activity

Description Baloxavir marboxil(S-033188), a cap-endonuclease inhibitor, is an antiviral drug.
In Vivo
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].

Animal Research Animal Models Specific-pathogen-free, 6-week-old BALB/c mice
Dosages 0.5, 1.5, 15 or 50 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06094010 Recruiting
Influenza
Hoffmann-La Roche
November 22 2023 Phase 3
NCT03653364 Completed
Influenza
Hoffmann-La Roche
January 23 2019 Phase 3
NCT03629184 Completed
Influenza
Hoffmann-La Roche
November 20 2018 Phase 3

Chemical Information & Solubility

Molecular Weight 571.55 Formula

C27H23F2N3O7S

CAS No. 1985606-14-1 SDF --
Smiles COC(=O)OCOC1=C2C(=O)N3CCOCC3N(N2C=CC1=O)C4C5=C(CSC6=CC=CC=C46)C(=C(C=C5)F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (174.96 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


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In vivo
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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.

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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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