Daptomycin

Catalog No.S1373 Synonyms: LY146032

Daptomycin Chemical Structure

Molecular Weight(MW): 1620.67

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

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Cited by 11 Publications

3 Customer Reviews

  • Same experiment as in Figure 2 with fluorescent daptomycin shown as confocal images. A 7/3 DOPC/DOPG GUV (including 1% Rh-PE) was introduced at time zero into a solution containing 1 uM daptomycin with 0.5 uM BODIPY-daptomycin and 1 mM Ca2+. To show colocalization of lipid and peptide in aggregates, confocal images were taken: red for RH-PE and green for BODIPY-daptomycin. As the protrusion length decreased, aggregates appeared on the GUV surface containing both lipid and peptide. The scale bar is 10 um.

    Biochemistry 2014 53(33), 5384-92. Daptomycin purchased from Selleck.

    Stoichiometry of daptomycin and calcium binding to PG-containing membranes. The experimental data are the fraction of 40 μM daptomycin in the B state, ϕ, as a function of Ca2+ concentration at different lipid concentrations. The lipids were DOPC/DOPG 7:3 in SUVs. The error bars represent the range of reproducibility for three independent measurements.

    Biophys J, 2017, 113(1):82-90. Daptomycin purchased from Selleck.

  • Membrane permeability induced by CCCP and daptomycin in E. coli spheroplasts. Experiments were conducted as described in Fig. 1a, but with different chemicals or fluorescent dyes. (a) Calcein and sytox orange (SO) permeability induced by CCCP (100 µM) in E. coli membranes is shown. The SO signal is represented as an increase from the initial state, (F-F0)/F0. (b) Calcein permeability induced by 1 µM daptomycin with 1 mM CaCl2.

    Biophys J, 2017, 112(8):1663-1672. Daptomycin purchased from Selleck.

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Biological Activity

Description Daptomycin is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.
Targets
DNA synthesis [1]
(Cell-free assay)
In vitro

Daptomycin (5 μg/ml) reduces cell viability by >99% and membrane potential by >90% within 30 min in Staphylococcus aureus. Daptomycin exhibits rapid in vitro bactericidal activity against clinically significant strains of gram-positive pathogens including hemolytic streptococci, methicillin-resistant Staphylococcus aureus, and vancomycin-resistant enterococci. Daptomycin acts at the cytoplasmic membrane of susceptible bacteria (8), as demonstrated by binding and fractionation studies. Daptomycin also differs from that of some antimicrobial peptides (e.g., human neutrophil peptide 1) that are capable of rapid depolarization of the cytoplasmic membrane but do not induce cell death for 1 hour to 2 hours. Daptomycin inserts into the cytoplasmic membrane of bacteria, as indicated by whole-cell and artificial membrane studies. [1] Daptomycin demonstrates greater bactericidal activity than all other drugs tested, killing ≥3 log CFU/ml by 8 hours. Daptomycin is a cyclic polypeptide derived from Streptomyces roseosporus and representing a class of antimicrobial agents known as the peptolides (acid lipopeptide antibiotics). Daptomycin is also active against vancomycin-resistant gram-positive bacteria, including enterococci. Daptomycin is highly protein bound (94%), and its in vitro activity is altered in the presence of serum or albumin.[2] Daptomycin consists of a 13-member amino acid cyclic lipopeptide with a decanoyl side-chain, the lipophilic Daptomycin tail into the bacterial cell membrane, causing rapid membrane depolarization and a potassium ion efflux. Daptomycin treatment has been linked to fully reversible skeletal muscle toxicity with no effect on smooth or cardiac muscle. [3]

In vivo Daptomycin exhibited linear pharmacokinetics, with an area under the concentration-time curve (AUC) from time zero to infinity/dose of 9.4 and a half-life of 0.9 to 1.4 h. The level of protein binding was 90%[5].

Protocol

Animal Research:

[4]

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  • Animal Models: ICR/Swiss mice
  • Formulation: saline
  • Dosages: 0, 1, 2.5, 5, 10, 15, or 20 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (61.7 mM)
Water 100 mg/mL warmed (61.7 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1620.67
Formula

C72H101N17O26

CAS No. 103060-53-3
Storage powder
in solvent
Synonyms LY146032

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03134521 Unknown status -- Bone Infection|Joint Infection Hospices Civils de Lyon December 1 2016 --
NCT03004066 Completed Drug: Daptomycin Heart Assist Device University Hospital Tuebingen October 2016 --
NCT03209921 Completed -- Bone and Joint Infection|Patient Treated by Daptomycin Hospices Civils de Lyon May 2015 --
NCT02241941 Withdrawn Drug: Daptomycin Burn Injury University of Zurich September 2014 Phase 4
NCT03209934 Completed -- Bone and Joint Infection|Treated by Daptomycin Hospices Civils de Lyon July 2014 --
NCT02097953 Completed Drug: Daptomycin|Drug: Rifampin Drug Interactions|Pharmacokinetics University of Utah|Cubist Pharmaceuticals LLC May 2014 Early Phase 1

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Frequently Asked Questions

  • Question 1:

    Could you tell me the native source for this product?

  • Answer:

    Daptomycin was synthesed from S.reseosporus.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID