Augpenin
Based on 1 Customer Validation
Augpenin (Ticarcillin-clavulanic acid mixt.; BRL28500) is a compound β-lactam antibacterial mixture of Ticarcillin (HY-139805) and Clavulanic acid (HY-A0256) in a 15:1 ratio. Ticarcillin in Augpenin acts on bacterial penicillin-binding proteins, while Clavulanic acid acts as an irreversible β-lactamase inhibitor that protects Ticarcillin from hydrolysis and restores its inhibitory activity against resistant strains. Augpenin significantly reduces the bacterial load of Legionella pneumophila in lung tissue of Cyclophosphamide (HY-17420)-induced neutropenic young rats. Augpenin can be used in research related to bacterial infections.
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- CAS No.: 86482-18-0
- Formule: C23H25N3O11S2
- Masse moléculaire:583.59
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Stockage:Powder -20°C, 3 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
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Activité biologique
Description
In Vitro
Augpenin (Ticarcillin-clavulanic acid) increases the susceptibility of many β-lactamase-producing aerobic and anaerobic bacteria to Ticarcillin (HY-139805), although P. aeruginosa remains highly resistant[1].
Augpenin exhibits high in vitro activity against a variety of anaerobic bacteria, and Clavulanic acid (HY-A0256) extends the activity spectrum of Ticarcillin to cover the B. fragilis group and enhances the activity of Ticarcillin against Methicillin (HY-121544)-sensitive and methicillin-resistant staphylococci[1].
Augpenin (BRL28500) (18 h) exhibits potent antibacterial activity against beta-lactamase-producing E. coli, K. pneumoniae, and S. aureus strains, with MIC values of 50, 100, 12.5, 50, and 25 μg/mL against E. coli 33, E. coli 113, K. pneumoniae 102, K. pneumoniae 200, and S. aureus L-5, respectively[2].
Augpenin (6.25-100 μg/mL) exhibits strong lytic activity against E. coli 33, K. pneumoniae 200, and S. aureus L-5, with effects observed at concentrations equal to or below the MIC[2].
Augpenin (6 h) protects TIPC from hydrolysis by beta-lactamases in cultures of E. coli 33, K. pneumoniae 200, and S. aureus L-5[2].
Augpenin (3.13-50 μg/mL; 3 h) primarily induces filamentous morphological changes in E. coli 33 and K. pneumoniae 200[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Augpenin (Ticarcillin-clavulanic acid) (200-600 mg/kg; subcutaneous injection; four times daily; 4 days) produces a bactericidal effect against L. pneumophila pneumonia in neutropenic weanling rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD (weanling male, 60-80 g, neutropenic via Cyclophosphamide (HY-17420), Legionella pneumophila pneumonia model)[3]
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Dosage:Ticarcillin 200 + Clavulanic acid 10 mg/kg
Ticarcillin 200 + Clavulanic acid 100 mg/kg
Ticarcillin 600 + Clavulanic acid 20 mg/kg
Ticarcillin 600 + Clavulanic acid 40 mg/kg -
Administration:s.c.; four times daily; 4 days
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Result:Reduced lung bacterial counts to 2.4 log10 CFU/g at 200 + 100 mg/kg, 3.6 log10 CFU/g at 600 + 20 mg/kg, and 2.5 log10 CFU/g at 600 + 40 mg/kg at 96 h postinfection.
Chemical Information
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CAS No. 86482-18-0
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Appearance Solid
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Masse moléculaire 583.59
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Formule C23H25N3O11S2
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Color White to light yellow
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SMILES
OC([C@H](C1=CSC=C1)C(N[C@H]2[C@]3([H])N(C2=O)[C@H](C(C)(S3)C)C(O)=O)=O)=O.OC([C@@H]4N5[C@](CC5=O)([H])O/C4=C\CO)=O
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Synonyms
Ticarcillin-clavulanic acid mixt.; BRL28500
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (171.35 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 (4.28 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 (4.28 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 (288 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 1.7135 mL | 8.5677 mL | 17.1353 mL | 42.8383 mL |
| 5 mM | 0.3427 mL | 1.7135 mL | 3.4271 mL | 8.5677 mL | |
| 10 mM | 0.1714 mL | 0.8568 mL | 1.7135 mL | 4.2838 mL | |
| 15 mM | 0.1142 mL | 0.5712 mL | 1.1424 mL | 2.8559 mL | |
| 20 mM | 0.0857 mL | 0.4284 mL | 0.8568 mL | 2.1419 mL | |
| 25 mM | 0.0685 mL | 0.3427 mL | 0.6854 mL | 1.7135 mL | |
| 30 mM | 0.0571 mL | 0.2856 mL | 0.5712 mL | 1.4279 mL | |
| 40 mM | 0.0428 mL | 0.2142 mL | 0.4284 mL | 1.0710 mL | |
| 50 mM | 0.0343 mL | 0.1714 mL | 0.3427 mL | 0.8568 mL | |
| 60 mM | 0.0286 mL | 0.1428 mL | 0.2856 mL | 0.7140 mL | |
| 80 mM | 0.0214 mL | 0.1071 mL | 0.2142 mL | 0.5355 mL | |
| 100 mM | 0.0171 mL | 0.0857 mL | 0.1714 mL | 0.4284 mL |
Augpenin Related Classifications
HY-156264 Related Classifications
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Keywords
- Augpenin
- 86482-18-0
- Ticarcillin-clavulanic acid mixt.
- BRL28500
- BRL28500
- BRL 28500
- BRL-28500
- Bacterial
- Beta-lactamase
- beta-lactamase inhibitor
- PBP 2
- Bacteroides fragilis group anaerobes
- Legionella pneumophila beta-lactamase
- plasmid-mediated S. aureus beta-lactamase
- Richmond and Sykes classes II-VI beta-lactamases
- Legionella pneumophila pneumonia
- PBP 3
- P. aeruginosa
- penicillin-binding proteins
- Inhibitor
- inhibitor
- inhibit