Name | bc-3781 |
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Synonyms | 14-O-{[(1R,2R,4R)-4-amino-2-hydroxy-cyclohexylsulfanyl]-acetyl}-mutilin |
Description | 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[1]. |
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Related Catalog | |
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]. Cell Viability Assay[1] 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. |
In Vivo | Lefamulin (10-140 mg/kg, s.c.) shows anti-inflammatory effect on LPS-induced lung neutrophilia mouse model[4]. Lefamulin (1.25-160 mg/kg, s.c.) shows antibacterial effect in S. pneumoniae or S. aureus challenged lung infection mice[5]. Animal Model: LPS-induced lung neutrophilia mouse model[4] 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. |
Molecular Formula | C28H45NO5S |
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Molecular Weight | 507.72600 |
Exact Mass | 507.30200 |
PSA | 135.15000 |
LogP | 4.56710 |