Daptomycin

Research use only, not for human use.

Daptomycin is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.

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.

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.

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.

Cubicin | LY146032

Cell Cycle/DNA Damage

DNA/RNA Synthesis

DNA synthesis

Infection

——

103060-53-3

1620.68

C72H101N17O26

>98% (HPLC)

Water: 100 mg/mL (61.7 mM)

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

2,2'-((3S,6S,9R,15S,18R,21S,24S)-30-((S)-2-((S)-4-amino-2-((S)-2-decanamido-3-(1H-indol-3-yl)propanamido)-4-oxobutanamido)-3-carboxypropanamido)-3-(2-(2-aminophenyl)-2-oxoethyl)-24-(3-aminopropyl)-6-((R)-1-carboxypropan-2-yl)-9-(hydroxymethyl)-18,31-dimethyl-2,5,8,11,14,17,20,23,26,29-decaoxo-1-oxa-4,7,10,13,16,19,22,25,28-nonaazacyclohentriacontane-15,21-diyl)diacetic acid

(-20℃)

With Ice Pack

≥ 2 years