Lefamulin

SKU: orb1219145

Description

Lefamulin is a semi-synthetic compound that inhibits the synthesis of bacterial protein, which is required for bacteria to grow.(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.(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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1061337-51-6
• MW: 507.3
• Purity: >98% (HPLC)
• Formula: C₂₈H₄₅NO₅S
• SMILES: O=C(O[C@H]1[C@@]([C@H](C)CC2)(C)[C@@](C(CC3)=O)([H])[C@]32[C@@H](C)[C@H](O)[C@](C)(C=C)C1)CS[C@H]4[C@H](O)C[C@H](N)CC4
• Target: Others
• Solubility: DMSO:10 mM

Bioactivity

• In Vivo:
  Lefamulin (10-140 mg/kg, s. c.) shows anti-inflammatory effect on LPS-induced lung neutrophilia mouse model. Lefamulin (1.25-160 mg/kg, s. c.) 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.
  Read more...
• In Vitro:
  Lefamulin (0-1 mg/L) shows inhibitory activity against C. trachomatis, N. gonorrhoeae, and M. genitalium. Lefamulin 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.
  Read more...

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

Quick Database Links

Gene Symbol

Others