1. Anti-infection
  2. Influenza Virus
  3. Baloxavir

Baloxavir  (Synonyms: Baloxavir acid; S-033447)

Cat. No.: HY-109025A Purity: 99.68%
COA Handling Instructions

Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity.

For research use only. We do not sell to patients.

Baloxavir Chemical Structure

Baloxavir Chemical Structure

CAS No. : 1985605-59-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 222 In-stock
Solution
10 mM * 1 mL in DMSO USD 222 In-stock
Solid
5 mg USD 209 In-stock
10 mg USD 330 In-stock
25 mg USD 638 In-stock
50 mg USD 900 In-stock
100 mg USD 1440 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of Baloxavir:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity[1][2].

IC50 & Target

Influenza virus[1] Cap-dependent endonuclease (CEN)[1][2]

In Vitro

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 (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. Baloxavir 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) 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].
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. 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

483.49

Formula

C24H19F2N3O4S

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1N2[C@](COCC2)([H])N([C@@H]3C4=CC=CC=C4SCC5=C(F)C(F)=CC=C35)N6C1=C(O)C(C=C6)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 1 years; -20°C, 6 months (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (86.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0683 mL 10.3415 mL 20.6830 mL
5 mM 0.4137 mL 2.0683 mL 4.1366 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 1 years; -20°C, 6 months (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.68%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0683 mL 10.3415 mL 20.6830 mL 51.7074 mL
5 mM 0.4137 mL 2.0683 mL 4.1366 mL 10.3415 mL
10 mM 0.2068 mL 1.0341 mL 2.0683 mL 5.1707 mL
15 mM 0.1379 mL 0.6894 mL 1.3789 mL 3.4472 mL
20 mM 0.1034 mL 0.5171 mL 1.0341 mL 2.5854 mL
25 mM 0.0827 mL 0.4137 mL 0.8273 mL 2.0683 mL
30 mM 0.0689 mL 0.3447 mL 0.6894 mL 1.7236 mL
40 mM 0.0517 mL 0.2585 mL 0.5171 mL 1.2927 mL
50 mM 0.0414 mL 0.2068 mL 0.4137 mL 1.0341 mL
60 mM 0.0345 mL 0.1724 mL 0.3447 mL 0.8618 mL
80 mM 0.0259 mL 0.1293 mL 0.2585 mL 0.6463 mL
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Baloxavir Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Baloxavir
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