TXA707
Based on 1 Customer Validation
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.64%
- CAS No.: 1609670-89-4
- Formule: C15H8F5N3O2S
- Masse moléculaire:389.30
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR/Swiss (6-week-old, female, specific pathogen-free, 23 to 27 g, neutropenic model induced by intraperitoneal cyclophosphamide)[2]
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Dosage:20 mg/kg; 40 mg/kg; 80 mg/kg; 160 mg/kg
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Administration:p.o.; 6-, 8-, 12-, or 24-hour dosing intervals over 24 hours
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Result:Achieved an MIC of 1 mg/L against all 5 Staphylococcus aureus isolates.
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Animal Model:ICR/Swiss (6-week-old, female, specific pathogen-free, 23 to 27 g, neutropenic model induced by intraperitoneal cyclophosphamide)[2]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg; 80 mg/kg; 160 mg/kg
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Administration:p.o.; every 6 hours over 24 hours
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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.
Chemical Information
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CAS No. 1609670-89-4
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Appearance Solid
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Masse moléculaire 389.30
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Formule C15H8F5N3O2S
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Color Light yellow to yellow
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SMILES
O=C(C1=C(F)C(OCC2=NC3=C(S2)N=CC(C(F)(F)F)=C3)=CC=C1F)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ferrer-González E, et al. β-Lactam Antibiotics with a High Affinity for PBP2 Act Synergistically with the FtsZ-Targeting Agent TXA707 against Methicillin-Resistant Staphylococcus aureus. Antimicrob Agents Chemother. 2017;61(9):e00863-17. Published 2017 Aug 24. [Content Brief]
[2]. Lepak AJ, et al. In Vivo Pharmacodynamic Evaluation of an FtsZ Inhibitor, TXA-709, and Its Active Metabolite, TXA-707, in a Murine Neutropenic Thigh Infection Model. Antimicrob Agents Chemother. 2015 Oct;59(10):6568-74. [Content Brief]
[3]. Kaul M, et al. TXA709, an FtsZ-Targeting Benzamide Prodrug with Improved Pharmacokinetics and Enhanced In Vivo Efficacy against Methicillin-Resistant Staphylococcus aureus. Antimicrob Agents Chemother. 2015 Aug;59(8):4845-55. [Content Brief]
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 |
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| 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 |
TXA707 Related Classifications
HY-153695 Related Classifications
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