Lefamulin acetate

Research use only, not for human use.

Lefamulin acetate (BC-3781 acetate) is the first semi-synthetic pleuromutilin for systemic treatment of bacterial infections in humans.

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).

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.

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.

BC-3781 acetate

Microbiology/Virology

ribosome

VHL

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1350636-82-6

567.78

C30H49NO7S

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (176.12 mM)

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

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(-20℃)

With Ice Pack

≥ 2 years