Lefamulin acetate
Lefamulin acetate Basic information
- Product Name:
- Lefamulin acetate
- Synonyms:
-
- WSMXIQXWHPSVDE-WHAUHWDVSA-N
- BC-3781;BC 3781;BC3781
- Lefamulin acetate
- BC-3781 ACETATE
- Lefamulin acetate (BC-3781 acetate)
- WSMXIQXWHPSVDE-WHAUHWDVSA-N USP/EP/BP
- Inhibitor,Lefamulin,BC 3781,BC3781,Lefamulin acetate,inhibit,BC-3781,Bacterial,Antibiotic
- Lefamulin acetate (Xenleta)
- CAS:
- 1350636-82-6
- MF:
- C30H49NO7S
- MW:
- 567.78
- EINECS:
- 208-388-5
- Mol File:
- 1350636-82-6.mol
Lefamulin acetate Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO:100.0(Max Conc. mg/mL);176.12(Max Conc. mM)
- form
- Solid
- color
- White to off-white
- InChI
- InChI=1/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?;/s3
- InChIKey
- WSMXIQXWHPSVDE-IHBHSJRLNA-N
- SMILES
- C(=O)(O)C.C[C@H]1[C@@H]([C@](C[C@@H](OC(=O)CS[C@@H]2CC[C@@H](N)C[C@H]2O)C2([C@H](C)CCC31CCC(=O)[C@]32[H])C)(C)C=C)O |&1:5,6,7,9,15,18,21,24,33,r|
Lefamulin acetate Usage And Synthesis
Chemical Properties
Lefamulin acetate is a white to off-white solid. It is a stable compound (requiring no special storage conditions) which is highly soluble in water and 0.9% sodium chloride solution (>300mg/ml). The hydration level of lefamulin acetate at ambient conditions is typically below 1% w/w.
Uses
Lefamulin (BC-3781) acetate is an orally active antibiotic. Lefamulin acetate inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome. Lefamulin acetate has anti-inflammatory activity. Lefamulin acetate can be used in the research of bacterial infections, such as bacterial pneumonia.
Definition
Lefamulin acetate is a single stereoisomer semi-synthetically derived from pleuromutilin, a homochiral, natural fermentation product of known absolute stereochemistry. Lefamulin acetate is a diastereomer with R-configuration at carbons of the cyclohexane moiety. The absolute configuration of the active substance has been confirmed by single-crystal structure determination.
Antimicrobial activity
Lefamulin acetate has activity against Gram-positive bacteria including MRSA, and atypical bacteria, especially those causing CAPB (i.e. Streptococcus pneumonia, Haemophilus influenzae, Mycoplasma pneumoniae, Legionella pneumophila, Chlamydophila pneumoniae). It also has activity against Gram-negative organisms.
in vivo
Lefamulin (10-140 mg/kg, s.c.) acetate shows anti-inflammatory effect on LPS-induced lung neutrophilia mouse model[4].
Lefamulin (1.25-160 mg/kg, s.c.) acetate shows antibacterial effect in S. pneumoniae or S. aureus challenged lung infection mice[5].
| 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. |
Lefamulin acetateSupplier
- Tel
- 18915538011; 18915538011
- liwei@boyanpharma.com
- Tel
- 028-86136736 19130631884
- sales@mic-pharma.com
- Tel
- 13568817957
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- 0556-5032306 18917961636
- wtx@bayeebio.com
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- 15301951213
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