Daptomycin

SKU: orb1227114

Description

Daptomycin is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.(In Vitro):Daptomycin has excellent in-vitro inhibitory and bactericidal activity against nafcillin-susceptible and resistant staphylococci (MIC90 less than or equal to 0.5 mg/L) and against enterococci (MIC90 less than or equal to 2.0 mg/L). Daptomycin is more active than vancomycin against the majority of isolated tested. With the exception of trimethoprim-sulphamethoxazole, daptomycin is the most active agent in vitro against enterococci, and is the most active against nafcillin-resistant staphylococci. Daptomycin and vancomycin show a marked increase in MIC when the inoculum is increased from 105 to 107 cfu/mL. Daptomycin is effective within a very narrow range of drug concentrations (from 0.125 to 2.0 tLg/mL) and is more active than other agents tested against S. faecalis. Daptomycin inhibits the formation of these nucleotide-linked intermediates.(In Vivo):At a dose of 10 mg/kg given twice daily, daptomycin reduces the number of organisms per kidney significantly compared with that in infected untreated controls within 48 h after the initiation of therapy. At 20 mg/kg given once a day, daptomycin is less effective but reduces colony counts significantly after 4 days of therapy, and its activity is comparable to that of vancomycin or vancomycin-gentamicin given twice daily.

Key Properties

• CAS Number: 103060-53-3
• MW: 1620.68
• Purity: >98% (HPLC)
• Formula: C₇₂H₁₀₁N₁₇O₂₆
• SMILES: O=C1NCC(N[C@@H](CCCN)C(N[C@@H](CC(O)=O)C(N[C@H](C)C(N[C@@H](CC(O)=O)C(NCC(N[C@H](CO)C(N[C@@H]([C@H](C)CC(O)=O)C(N[C@@H](CC(C2=CC=CC=C2N)=O)C(OC(C)C1NC([C@@H](NC([C@@H](NC([C@@H](NC(CCCCCCCCC)=O)CC3=CNC4=C3C=CC=C4)=O)CC(N)=O)=O)CC(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
• Target: DNA/RNA Synthesis
• Solubility: Water: 100 mg/mL (61.7 mM)

Bioactivity

• In Vivo:
  At a dose of 10 mg/kg given twice daily, daptomycin reduces the number of organisms per kidney significantly compared with that in infected untreated controls within 48 h after the initiation of therapy. At 20 mg/kg given once a day, daptomycin is less effective but reduces colony counts significantly after 4 days of therapy, and its activity is comparable to that of vancomycin or vancomycin-gentamicin given twice daily.
• In Vitro:
  Daptomycin has excellent in-vitro inhibitory and bactericidal activity against nafcillin-susceptible and resistant staphylococci (MIC90 less than or equal to 0.5 mg/L) and against enterococci (MIC90 less than or equal to 2.0 mg/L). Daptomycin is more active than vancomycin against the majority of isolated tested. With the exception of trimethoprim-sulphamethoxazole, daptomycin is the most active agent in vitro against enterococci, and is the most active against nafcillin-resistant staphylococci. Daptomycin and vancomycin show a marked increase in MIC when the inoculum is increased from 105 to 107 cfu/mL. Daptomycin is effective within a very narrow range of drug concentrations (from 0.125 to 2.0 tLg/mL) and is more active than other agents tested against S. faecalis. Daptomycin inhibits the formation of these nucleotide-linked intermediates.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cubicin | LY146032

Quick Database Links

Gene Symbol

DNA/RNA Synthesis