DC Chemicals · Product datasheet

Lefamulin acetate — Datasheet

CAT. NO. DC12387

Product page and current package options

ParameterValue
Chemical Name(3aS,4R,5S,6S,8R,9R,9aR,10R)-6-ethenyl-5-hydroxy-4,6,9,10-tetramethyl-1-oxodecahydro-3a,9-propano-3aH-cyclopenta[8]annulen-8-yl {[(1R,2R,4R)-4-amino-2-hydroxycyclohexyl]sulfanyl}acetate
CAS No.1350636-82-6
SynonymsBC-3781,BC 3781,BC3781
FormulaC30H47NO6S
M.Wt549.76
SMILESO=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](OC(C)=O)C[C@H](N)CC4
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Lefamulin acetate (BC-3781 acetate) is an orally active antibiotic for community-acquired bacterial pneumonia (CABP) treatment. 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[1].

In Vitro

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)[1]. 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)[1].

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

[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.

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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