1. Anti-infection
  2. Bacterial
  3. TXA707

TXA707 is an FtsZ-targeting antibacterial agent. TXA707 disrupts bacterial septum formation, induces cell enlargement, causes penicillin-binding protein mislocalization, and triggers cell lysis in Staphylococcus aureus cells. TXA707 can be used for the research of Staphylococcus aureus infections.

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

TXA707

TXA707 Chemical Structure

CAS No. : 1609670-89-4

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Description

TXA707 is an FtsZ-targeting antibacterial agent. TXA707 disrupts bacterial septum formation, induces cell enlargement, causes penicillin-binding protein mislocalization, and triggers cell lysis in Staphylococcus aureus cells. TXA707 can be used for the research of Staphylococcus aureus infections[1][2][3].

In Vitro

TXA707 (2 μg/mL; 24 h) potently inhibits MRSA COL growth with an MIC of 2 μg/mL[1].
TXA707 (24 h) acts synergistically with all tested β-lactam antibiotics to exert bactericidal activity against MRSA COL[1].
TXA707 (3 h) disrupts septum formation and induces peripheral cell wall invaginations in MRSA COL cells[1].
TXA707 (3 h) disrupts septum formation in MRSA COL cells by mislocalizing PBPs from midcell septa to nonproductive peripheral sites[1].
TXA707 (1 mg/L) inhibits the growth of Methicillin (HY-121544)-susceptible and Methicillin-resistant Staphylococcus aureus isolates in vitro with an MIC of 1 mg/L[2].
TXA707 (16-24 h) exhibits potent bactericidal activity against all tested clinical and laboratory Staphylococcus aureus isolates, including those resistant to Vancomycin (HY-B0671), Daptomycin (HY-B0108), or Linezolid (HY-10394), with a consistent modal MIC50 of 1 µg/mL[3].
TXA707 (0.5-5 µg/mL) concentration-dependently stimulates polymerization of purified S. aureus FtsZ, with maximum activity observed at 5 µg/mL[3].
TXA707 (4 µg/mL; 2 h) inhibits cell division in Bacillus subtilis FG347 by disrupting FtsZ Z-ring formation[3].
TXA707 (4 µg/mL; 1, 4, or 9 h) disrupts septum formation and induces cell enlargement and lysis in MSSA 8325-4 cells[3].

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

Parmacokinetics
Species Dose Route AUC0-∞ Cmax T1/2
Mice[2] 10 mg/kg p.o. 2.7 mg·h/L 0.5 mg/L 3.5 h
Mice[2] 40 mg/kg p.o. 28.1 mg·h/L 5.4 mg/L 3.2 h
Mice[2] 160 mg/kg p.o. 96.4 mg·h/L 13.7 mg/L 4.4 h
In Vivo

TXA707 (delivered via prodrug TXA-709) (2.5-160 mg/kg; p.o.) exhibits dose-dependent in vivo efficacy against methicillin-susceptible and resistant S. aureus isolates in a neutropenic murine thigh infection model, with a mean total drug 24-hour AUC/MIC of 122 required for net stasis and 243 required for 1-log10 bacterial kill, and AUC/MIC as the most predictive PD index[2].

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

Animal Model: ICR/Swiss (6-week-old, female, specific pathogen-free, 23 to 27 g, neutropenic model induced by intraperitoneal cyclophosphamide)[2]
Dosage: 20 mg/kg; 40 mg/kg; 80 mg/kg; 160 mg/kg
Administration: p.o.; 6-, 8-, 12-, or 24-hour dosing intervals over 24 hours
Result: Achieved an MIC of 1 mg/L against all 5 Staphylococcus aureus isolates.
Animal Model: ICR/Swiss (6-week-old, female, specific pathogen-free, 23 to 27 g, neutropenic model induced by intraperitoneal cyclophosphamide)[2]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg; 80 mg/kg; 160 mg/kg
Administration: p.o.; every 6 hours over 24 hours
Result: Demonstrated dose-dependent efficacy, with net stasis achieved against all isolates and 1-log10 bacterial kill achieved against 4 of 5 isolates.
Revealed a mean total drug 24-hour AUC/MIC of 122 (free drug AUC/MIC = 17.1) for net stasis, and a mean total drug 24-hour AUC/MIC of 243 (free drug AUC/MIC = 34) for 1-log10 kill.
Identified AUC/MIC as the PD index most closely linked to efficacy (R2 = 0.72 for the dose-fractionation study, R2 = 0.74 across all isolates).
Showed beta-lactam resistance did not alter potency or PD targets.
Molecular Weight

389.30

Formula

C15H8F5N3O2S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(F)C(OCC2=NC3=C(S2)N=CC(C(F)(F)F)=C3)=CC=C1F)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (256.87 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 2.5687 mL 12.8436 mL 25.6871 mL
5 mM 0.5137 mL 2.5687 mL 5.1374 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

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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: ≥ 2.5 mg/mL (6.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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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).
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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5687 mL 12.8436 mL 25.6871 mL 64.2178 mL
5 mM 0.5137 mL 2.5687 mL 5.1374 mL 12.8436 mL
10 mM 0.2569 mL 1.2844 mL 2.5687 mL 6.4218 mL
15 mM 0.1712 mL 0.8562 mL 1.7125 mL 4.2812 mL
20 mM 0.1284 mL 0.6422 mL 1.2844 mL 3.2109 mL
25 mM 0.1027 mL 0.5137 mL 1.0275 mL 2.5687 mL
30 mM 0.0856 mL 0.4281 mL 0.8562 mL 2.1406 mL
40 mM 0.0642 mL 0.3211 mL 0.6422 mL 1.6054 mL
50 mM 0.0514 mL 0.2569 mL 0.5137 mL 1.2844 mL
60 mM 0.0428 mL 0.2141 mL 0.4281 mL 1.0703 mL
80 mM 0.0321 mL 0.1605 mL 0.3211 mL 0.8027 mL
100 mM 0.0257 mL 0.1284 mL 0.2569 mL 0.6422 mL
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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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