Lolamicin
Based on 1 Customer Validation
Lolamicin is an orally effective inhibitor that specifically targets the Gram-negative bacteria lipoprotein transport system LolCDE complex. It selectively inhibits the transmembrane transport of outer membrane lipoproteins by competitively binding to lipoprotein binding sites. Lolamicin destroys the integrity of the bacterial outer membrane, leading to cell death, and has both bactericidal and antibacterial activity. It has significant effects on multidrug-resistant Enterobacteriaceae pathogens (such as Escherichia coli and Klebsiella pneumoniae). Lolamicin can be used to inhibit the study of acute pneumonia, sepsis and other infections caused by Gram-negative bacteria.
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- Pureza: 99.54%
- No. CAS: 2930690-12-1
- Fòrmula: C24H20N4O
- Peso molecular:380.44
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
In in vitro antibacterial experiments against Gram-negative bacteria (such as Escherichia coli, Klebsiella pneumoniae, and Enterobacter cloacae), Lolamicin (1-8 μg/mL; overnight culture) significantly reduces bacterial survival by inhibiting the lipoprotein transport system LolCDE[1].
In drug-resistant mutation screening experiments, Lolamicin (8×MIC; 2-48 h) induces LolC/LolE protein mutations (such as E195K, D264N) in Escherichia coli, Klebsiella pneumoniae, and Enterobacter cloacae, and the mutants are significantly less sensitive to lolamicin[1].
Lolamicin (3×MIC; 1.5 h) induces swelling of wild-type Escherichia coli and Klebsiella pneumoniae cells in confocal microscopy observation experiments, while resistant mutants (such as LolC-N265K and LolE-D264N) does not show this phenotype, indicating that it destroys the integrity of the outer membrane by interfering with lipoprotein transport[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Lolamicin (200 mg/kg; oral gavage; twice daily; 3 d) reduces lung tissue bacterial load and increases sepsis survival rate to more than 70% in acute pneumonia and sepsis models induced by Escherichia coli (AR0349) in male CD-1 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2930690-12-1
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Appearance Solid
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Peso molecular 380.44
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Fòrmula C24H20N4O
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Color Light yellow to yellow
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SMILES
N#CC1=CC=CC(COC2=CC=CC(C3=NNC=C3C4=CC(C)=NC(C)=C4)=C2)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 175 mg/mL (459.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : ≥ 100 mg/mL (262.85 mM)
* "≥" means soluble, but saturation unknown.
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)
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: ≥ 5 mg/mL (13.14 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Pureza y Documentación
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Ficha de datos (275 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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Instrucciones de manejo (2659 KB)
Referencias
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 |
|---|---|---|---|---|---|
| DMF / DMSO | 1 mM | 2.6285 mL | 13.1427 mL | 26.2854 mL | 65.7134 mL |
| 5 mM | 0.5257 mL | 2.6285 mL | 5.2571 mL | 13.1427 mL | |
| 10 mM | 0.2629 mL | 1.3143 mL | 2.6285 mL | 6.5713 mL | |
| 15 mM | 0.1752 mL | 0.8762 mL | 1.7524 mL | 4.3809 mL | |
| 20 mM | 0.1314 mL | 0.6571 mL | 1.3143 mL | 3.2857 mL | |
| 25 mM | 0.1051 mL | 0.5257 mL | 1.0514 mL | 2.6285 mL | |
| 30 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1904 mL | |
| 40 mM | 0.0657 mL | 0.3286 mL | 0.6571 mL | 1.6428 mL | |
| 50 mM | 0.0526 mL | 0.2629 mL | 0.5257 mL | 1.3143 mL | |
| 60 mM | 0.0438 mL | 0.2190 mL | 0.4381 mL | 1.0952 mL | |
| 80 mM | 0.0329 mL | 0.1643 mL | 0.3286 mL | 0.8214 mL | |
| 100 mM | 0.0263 mL | 0.1314 mL | 0.2629 mL | 0.6571 mL |
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