Daptomycin (LY146032)

Catalog No.S1373

For research use only.

Daptomycin (LY146032) is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.

Daptomycin (LY146032) Chemical Structure

CAS No. 103060-53-3

Selleck's Daptomycin (LY146032) has been cited by 19 publications

Purity & Quality Control

Choose Selective Antibiotics for Mammalian Cell Culture Inhibitors

Biological Activity

Description Daptomycin (LY146032) 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP-1 NG\OZnNCdnSrYnHjeIVzcWGuIHHzd4F6 NYjQUZp7SW62aXLhZ5RmemmjbDDhZ5Rqfmm2eTDh[4FqdnO2IGP0ZZBpgWyxY3;jZ5V{KGG3cnX1d{BUS1ZiaYPvcIF1\WRiZoLvcUBkgXO2aXOg[oljem:|aYOgdIF1cWWwdDDpcoZm[3SnZDDpckBpfW2jbjDUTHAuOSClZXzsd{Bie3Onc4Pl[EBieyCub3egdoVlfWO2aX;uJI9nKGmwdILhZ4VtdHWuYYKgR2ZWKGyndnXsJIFnfGW{IEK0JIhzeyCrbjDwdoV{\W6lZTDv[kB1cHmvaXTpcoU> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTF6OEO5N{c,OTlzOEizPVM9N2F-
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 Research:

[4]

  • Animal Models: ICR/Swiss mice
  • Dosages: 0, 1, 2.5, 5, 10, 15, or 20 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 1620.67
Formula

C72H101N17O26

CAS No. 103060-53-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCCCCCCC(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)O)C(=O)NC3C(OC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC3=O)CCCN)CC(=O)O)C)CC(=O)O)CO)C(C)CC(=O)O)CC(=O)C4=CC=CC=C4N)C

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04277143 Not yet recruiting Drug: Daptomycin Outcome Fatal|Infection Zhongnan Hospital December 1 2020 --
NCT04434300 Completed Drug: Daptomycin Antibiotics|Subcutaneous Injection|Daptomycin University Hospital Caen October 15 2020 Phase 1
NCT03643952 Completed Drug: Daptomycin for Injection Bacteremia|Soft Tissue Infections|Skin Diseases Infectious Merck Sharp & Dohme LLC December 6 2018 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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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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