Lefamulin
Based on 5 publication(s) in Google Scholar
Lefamulin (BC-3781) is an orally active antibiotic. Lefamulin inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome. Lefamulin has anti-inflammatory activity. Lefamulin can be used in the research of bacterial infections, such as bacterial pneumonia.
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- Pureté: 99.65%
- CAS No.: 1061337-51-6
- Formule: C28H45NO5S
- Masse moléculaire:507.73
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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
Publications Citing Use of MedChemExpress (MCE) Lefamulin
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Activité biologique
Description
In Vitro
Lefamulin (0-1 mg/L) shows inhibitory activity against C. trachomatis, N. gonorrhoeae, and M. genitalium[2].
Lefamulin shows potent activity against all M. pneumoniae strains with MIC values of ≤0.008 μg/mL[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C. trachomatis, N. gonorrhoeae, and M. genitalium
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Concentration:0-1 mg/L
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Incubation Time:
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Result:Inhibited bacterial activity with MIC50s of 0.02 mg/L, 0.063 mg/L and 0.12 mg/L respectively.
In Vivo
Lefamulin (1.25-160 mg/kg, s.c.) shows antibacterial effect in S. pneumoniae or S. aureus challenged lung infection mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS-induced lung neutrophilia mouse model[4]
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Dosage:10-140 mg/kg
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Administration:Subcutaneous injection (s.c.)
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Result:Reduced BALF neutrophil cell counts.
Reduced pro-inflammatory cytokine (TNF-α, IL-6, IL-1β, and GM-CSF), chemokine (CXCL-1, CXCL-2, and CCL-2) and MMP-9 levels in mouse lung tissue.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1061337-51-6
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Appearance Solid
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Masse moléculaire 507.73
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Formule C28H45NO5S
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Color White to off-white
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SMILES
C[C@@H]1[C@]23[C@](C(CC3)=O)([H])[C@]([C@@H](C[C@](C)([C@H]1O)C=C)OC(CS[C@H]4[C@@H](C[C@@H](CC4)N)O)=O)([C@@H](CC2)C)C
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Synonyms
BC-3781
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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
Publications (5)
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Journal Impact Factor
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Most Recent
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Microorganisms
In Vitro Synergistic Effect of Lefamulin with Doxycycline, Rifampin, and Quinupristin/Dalfopristin Against Enterococci. [Abstract]2024 Dec 6;12(12):2515. PMID: 39770718 -
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Antimicrob Agents Chemother
2021 Sep 17;65(10):e0061921. PMID: 34252305 -
J Antimicrob Chemother
Phenotypic antibiotic resistance of Mycoplasma genitalium and its variation between different macrolide resistance-associated mutations. [Abstract]2025 Feb 3;80(2):465-471. PMID: 39656801 -
Pathology
In vitro activity of recently introduced Gram-positive-specific antimicrobial agents against Australian methicillin-resistant Staphylococcus aureus isolates. [Abstract]2026 Feb 6:S0031-3025(26)00393-4. PMID: 41760492
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (196.96 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 (4.92 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 (4.92 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 (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Veve MP, et al. Lefamulin: Review of a Promising Novel Pleuromutilin Antibiotic. Pharmacotherapy. 2018 Sep;38(9):935-946. doi: 10.1002/phar.2166. Epub 2018 Aug 20. [Content Brief]
[2]. Susanne Paukner, et al. Antimicrob Agents Chemother. 2018 Apr 26;62(5):e02380-17. [Content Brief]
[3]. Ken B Waites, et al. In Vitro Activities of Lefamulin and Other Antimicrobial Agents against Macrolide-Susceptible and Macrolide-Resistant Mycoplasma pneumoniae from the United States, Europe, and China. Antimicrob Agents Chemother. 2017 Jan 24;61(2):e02008-16. [Content Brief]
[5]. Wolfgang W Wicha, et al. Pharmacokinetics/pharmacodynamics of lefamulin in a neutropenic murine pneumonia model with Staphylococcus aureus and Streptococcus pneumonia. J Antimicrob Chemother. 2019 Apr 1;74(Suppl 3):iii11-iii18. [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 | 1.9696 mL | 9.8478 mL | 19.6955 mL | 49.2388 mL |
| 5 mM | 0.3939 mL | 1.9696 mL | 3.9391 mL | 9.8478 mL | |
| 10 mM | 0.1970 mL | 0.9848 mL | 1.9696 mL | 4.9239 mL | |
| 15 mM | 0.1313 mL | 0.6565 mL | 1.3130 mL | 3.2826 mL | |
| 20 mM | 0.0985 mL | 0.4924 mL | 0.9848 mL | 2.4619 mL | |
| 25 mM | 0.0788 mL | 0.3939 mL | 0.7878 mL | 1.9696 mL | |
| 30 mM | 0.0657 mL | 0.3283 mL | 0.6565 mL | 1.6413 mL | |
| 40 mM | 0.0492 mL | 0.2462 mL | 0.4924 mL | 1.2310 mL | |
| 50 mM | 0.0394 mL | 0.1970 mL | 0.3939 mL | 0.9848 mL | |
| 60 mM | 0.0328 mL | 0.1641 mL | 0.3283 mL | 0.8206 mL | |
| 80 mM | 0.0246 mL | 0.1231 mL | 0.2462 mL | 0.6155 mL | |
| 100 mM | 0.0197 mL | 0.0985 mL | 0.1970 mL | 0.4924 mL |
Lefamulin Related Classifications
HY-16908 Related Classifications
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