Description
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.
Product information
CAS Number: 1350636-82-6
Molecular Weight: 567.78
Formula: C30H49NO7S
Chemical Name: (2R,3S,4S,6R,8R,14R)-4-ethenyl-3-hydroxy-2,4,7,14-tetramethyl-9-oxotricyclo[5.4.3.0¹,⁸]tetradecan-6-yl 2-{[(1R,2R,4R)-4-amino-2-hydroxycyclohexyl]sulfanyl}acetate; acetic acid
Smiles: CC(O)=O.C[C@]1(C[C@@H](OC(=O)CS[C@@H]2CC[C@@H](N)C[C@H]2O)C2(C)[C@@H]3C(=O)CCC3(CC[C@H]2C)[C@@H](C)[C@@H]1O)C=C
InChiKey: WSMXIQXWHPSVDE-WHAUHWDVSA-N
InChi: InChI=1S/C28H45NO5S.C2H4O2/c1-6-26(4)14-22(34-23(32)15-35-21-8-7-18(29)13-20(21)31)27(5)16(2)9-11-28(17(3)25(26)33)12-10-19(30)24(27)28;1-2(3)4/h6,16-18,20-22,24-25,31,33H,1,7-15,29H2,2-5H3;1H3,(H,3,4)/t16-,17+,18-,20-,21-,22-,24+,25+,26-,27?,28?;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 100 mg/mL (176.12 mM). H2O : < 0.1 mg/mL (insoluble).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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). 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).
Products are for research use only. Not for human use.
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