Lefamulin (Synonyms: BC-3781)

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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

CAS No. : 1061337-51-6

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Other Forms of Lefamulin:

Lefamulin acetate Get quote

1 Publications Citing Use of MCE Lefamulin

•Antimicrob Agents Chemother. 2021 Jul 12;AAC0061921. [Abstract]

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Biological Activity
Purity & Documentation
References
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Description

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.

1061337-51-6

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

Handling Instructions (2659 KB)

References

[1]. Veve MP, et al. Lefamulin: Review of a Promising Novel Pleuromutilin Antibiotic. Pharmacotherapy. 2018 Sep;38(9):935-946. doi: 10.1002/phar.2166. Epub 2018 Aug 20. [Content Brief]

[2]. Susanne Paukner, et al. Antimicrob Agents Chemother. 2018 Apr 26;62(5):e02380-17. [Content Brief]

[3]. Ken B Waites, et al. In Vitro Activities of Lefamulin and Other Antimicrobial Agents against Macrolide-Susceptible and Macrolide-Resistant Mycoplasma pneumoniae from the United States, Europe, and China. Antimicrob Agents Chemother. 2017 Jan 24;61(2):e02008-16. [Content Brief]

[4]. Michael Hafner, et al. Anti-inflammatory activity of lefamulin versus azithromycin and dexamethasone in vivo and in vitro in a lipopolysaccharide-induced lung neutrophilia mouse model. PLoS One. 2021 Sep 29;16(9): e0237659. https://pubmed.ncbi.nlm.nih.gov/34587166/

[5]. Wolfgang W Wicha, et al. Pharmacokinetics/pharmacodynamics of lefamulin in a neutropenic murine pneumonia model with Staphylococcus aureus and Streptococcus pneumonia. J Antimicrob Chemother. 2019 Apr 1;74(Suppl 3):iii11-iii18. [Content Brief]

Lefamulin Related Classifications

Infection

Molarity Calculator
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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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.

Keywords:

Lefamulin1061337-51-6BC-3781BC3781BC 3781BacterialAntibioticinfectionpneumoniapeptidyl transferaseneutrophiliainflammationInhibitorinhibitorinhibit

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