Daptomycin

Catalog No.S1373 Batch:S137312

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Technical Data

Formula

C72H101N17O26
Molecular Weight 1620.67 CAS No. 103060-53-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (61.7 mM)
Water 50 mg/mL (30.85 mM)
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.83mg/ml Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Animal Study:

[4]
  • Animal Models

    ICR/Swiss mice

  • Dosages

    0, 1, 2.5, 5, 10, 15, or 20 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by Biochemistry, 2014, 53(33), 5384-92]

Data from [Data independently produced by , , Biophys J, 2017, 113(1):82-90]

Data from [Data independently produced by , , Biophys J, 2017, 112(8):1663-1672]

Selleck's Daptomycin has been cited by 23 publications

Drug Metabolism of Hepatocyte-like Organoids and Their Applicability in In Vitro Toxicity Testing [ Molecules, 2023, 28(2)621] PubMed: 36677681
Efficacy of a Novel Antibacterial Agent Exeporfinium Chloride, (XF-73), Against Antibiotic-Resistant Bacteria in Mouse Superficial Skin Infection Models [ Infect Drug Resist, 2023, 16:4867-4879] PubMed: 37520450
Efficacy of a Novel Antibacterial Agent Exeporfinium Chloride, (XF-73), Against Antibiotic-Resistant Bacteria in Mouse Superficial Skin Infection Models [ Infect Drug Resist, 2023, 16:4867-4879] PubMed: 37520450
Targeted Killing of Staphylococcus aureus Using Specific Peptides Displayed on Yeast Vacuoles [ Microbiol Spectr, 2023, e0092023.] PubMed: 37098917
Potential drug discovery for COVID-19 treatment targeting Cathepsin L using a deep learning-based strategy [ Comput Struct Biotechnol J, 2022, 20:2442-2454] PubMed: 35602976
Daptomycin-Induced Lipid Phases on Model Lipid Bilayers: Effect of Lipid Type and of Lipid Leaflet Order on Membrane Permeability [ J Phys Chem B, 2021, 125(22):5775-5785] PubMed: 34038100
Identification of the Molecular Determinants Involved in Antimicrobial Activity of Pseudodesmin A, a Cyclic Lipopeptide From the Viscosin Group. [ Front Microbiol, 2020, 21;11:646] PubMed: 32373092
Antibacterial activity of novel dual bacterial DNA type II topoisomerase inhibitors. [ PLoS One, 2020, 15(2):e0228509] PubMed: 32074119
Globally deimmunized lysostaphin evades human immune surveillance and enables highly efficacious repeat dosing [ Sci Adv, 2020, 6(34):eaba8968] PubMed: 32917596
Violacein Targets the Cytoplasmic Membrane of Bacteria. [ ACS Infect Dis, 2019, 5(4):539-549] PubMed: 30693760

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.