1. Lefamulin

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Lefamulin acetate) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Lefamulin Chemical Structure

Lefamulin Chemical Structure

CAS No. : 1061337-51-6

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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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

507.73

Formula

C28H45NO5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H]1[C@]23[C@](C(CC3)=O)([H])[C@]([C@@H](C[C@](C)([C@H]1O)C=C)OC(CS[C@H]4[C@@H](C[C@@H](CC4)N)O)=O)([C@@H](CC2)C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Lefamulin
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HY-16908
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