Lefamulin

SKU: orb1299682

Description

Lefamulin is a semi-synthetic antibiotic that acts by inhibiting bacterial protein synthesis, thereby preventing bacterial growth. It is utilized in research for studying antibiotic resistance mechanisms and has demonstrated efficacy in both in vitro assays and in vivo models of bacterial infection.

Research Area

Infectious Disease & Virology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1061337-51-6
• MW: 507.73
• Purity: 99.63% (May vary between batches)
• Formula: C₂₈H₄₅NO₅S
• SMILES: C[C@@H]1[C@]23[C@]([C@](C)([C@H](OC(CS[C@H]4[C@H](O)C[C@H](N)CC4)=O)C[C@](C=C)(C)[C@H]1O)[C@H](C)CC2)(C(=O)CC3)[H]
• Target: Antibacterial,Others,Antibiotic
• Solubility: DMSO:50 mg/mL (98.48 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (4.92 mM)

Bioactivity

• In Vivo:
  Lefamulin exhibits a unique mechanism of action through inhibition of protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome, thus preventing the binding of transfer RNA for peptide transfer. Lefamulin displays activity against gram-positive and atypical organisms associated with CABP (i.e., Streptococcus pneumoniae, Haemophilus influenzae, Mycoplasma pneumoniae, Legionella pneumophila, and Chlamydophila pneumoniae), with an expanded gram-positive spectrum including Staphylococcus aureus (i.e., methicillin-resistant, vancomycin-intermediate, and heterogeneous strains) and vancomycin-resistant Enterococcus faecium. Lefamulin was also shown to retain activity against multidrug-resistant Neisseria gonorrhoeae and Mycoplasma genitalium. Lefamulin exhibits time-dependent killing, and the pharmacodynamic target best associated with antibacterial activity is AUC0-24 /MIC (minimum inhibitory concentration [MIC]).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Lefamulin, BC3781, BC-3781, BC 3781

Compound Identifiers

PubChem CID

25185057