Name: Baloxavir marboxil
Brand: Selleck Chemicals
SKU: S5952
Rating: 5 (2 reviews)

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.92

Related Targets	Integrase Bacterial Antibiotics Anti-infection Fungal COVID-19 Parasite Reverse Transcriptase HIV HCV Protease
Other Antiviral Inhibitors	Moroxydine HCl Aloperine GS-441524 Oleanolic Acid Harringtonine NGI-1 U18666A Aloin B Saikosaponin B2 Lapachol

Chemical Information, Storage & Stability

Molecular Weight	571.55	Formula	C₂₇H₂₃F₂N₃O₇S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1985606-14-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	S-033188			Smiles	COC(=O)OCOC1=C2C(=O)N3CCOCC3N(N2C=CC1=O)C4C5=C(CSC6=CC=CC=C46)C(=C(C=C5)F)F

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (174.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/ml (0.70mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.

Mechanism of Action

In vivo

Single-dose oral baloxavir marboxil is well tolerated, had a favourable safety profile, and has favourable 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 faecal excretion, whereas urinary excretion was low in rats and monkeys. 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.

References

[1] https://pubmed.ncbi.nlm.nih.gov/30184455/
[2] https://pubmed.ncbi.nlm.nih.gov/30476172/
[3] https://pubmed.ncbi.nlm.nih.gov/30288682/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Baloxavir marboxil Antiviral inhibitor

Chemical Structure

Molecular Weight: 571.55