Lefamulin acetate

SKU: orb1940791

Description

Lefamulin acetate (BC-3781 acetate) is the first semi-synthetic pleuromutilin for systemic treatment of bacterial infections in humans. Lefamulin acetate (BC-3781 acetate) inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome, preventing the binding of transfer RNA for peptide transfer. Lefamulin acetate (BC-3781 acetate) is an orally active antibiotic for community-acquired bacterial pneumonia (CABP) treatment.(In Vitro):Lefamulin has activity against gram-negative organisms, including Haemophilus influenza (MIC50=1 μg/ml; MIC90=0.12 μg/ml) and Moraxella cotarrhali (MIC50=2 μg/ml; MIC90=0.25 μg/ml).Lefamulin acetate (BC-3781 acetate) has activity against the resistant gram-postive organisms, including taphylococcus aureus (MRSA) (MIC50=0.12 μg/ml; MIC90=0.25 μg/ml); β-Hemolytic strepococcus (MIC50=0.03 μg/ml; MIC90=0.03 μg/ml); Viridans group Streptococcus (MIC50=0.12 μg/ml; MIC90=0.5 μg/ml), Enterocossus faecium (MIC50=0.12 μg/ml; MIC90=4 μg/ml), Streptococcus pneumonia (MIC50=0.12 μg/ml; MIC90 =0.25 μg/ml).

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1350636-82-6
• MW: 567.78
• Purity: >98% (HPLC)
• Formula: C₃₀H₄₉NO₇S
• SMILES: CC(O)=O.[H][C@@]12C(=O)CCC11CC[C@@H](C)C2(C)[C@@H](C[C@@](C)(C=C)[C@@H](O)[C@@H]1C)OC(=O)CS[C@@H]1CC[C@@H](N)C[C@H]1O
• Target: ribosome
• Solubility: In Vitro: DMSO : ≥ 100 mg/mL (176.12 mM)

Bioactivity

• In Vivo:
  Lefamulin (10-140 mg/kg, s. c.) acetate shows anti-inflammatory effect on LPS-induced lung neutrophilia mouse model. Lefamulin (1.25-160 mg/kg, s. c.) acetate shows antibacterial effect in S. pneumoniae or S. aureus challenged lung infection mice. Animal model: LPS-induced lung neutrophilia mouse model. Dosage: 10-140 mg/kg. Administration: Subcutaneous injection (s. c.). 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.
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• In Vitro:
  Lefamulin (0-1 mg/L) acetate shows inhibitory activity against C. trachomatis, N. gonorrhoeae, and M. genitalium. Lefamulin acetate shows potent activity against all M. pneumoniae strains with MIC values of ≤0.008 μg/mL. Cell Viability Assay Cell line: C. trachomatis, N. gonorrhoeae, and M. genitalium Concentration: 0-1 mg/L. Incubation time: Result: Inhibited bacterial activity with MIC50s of 0.02 mg/L, 0.063 mg/L and 0.12 mg/L respectively.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BC-3781 acetate

Quick Database Links

Gene Symbol

ribosome