Home DNA Damage/DNA Repair Antibiotics for Mammalian Cell Culture inhibitor - Bacterial chemical - DNA/RNA Synthesis inhibitor - Antibiotics chemical Daptomycin For research use only.

Daptomycin

Synonyms: LY146032

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

Daptomycin Chemical Structure

Daptomycin Chemical Structure

CAS No. 103060-53-3

Purity & Quality Control

Daptomycin Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP-1 Antibacterial assay Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level after 24 hrs in presence of thymidine 19188393
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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
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
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].
Animal Research Animal Models ICR/Swiss mice
Dosages 0, 1, 2.5, 5, 10, 15, or 20 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04277143 Unknown status
Outcome Fatal|Infection
Zhongnan Hospital
 December 1 2020 --
NCT04434300 Completed
Antibiotics|Subcutaneous Injection|Daptomycin
University Hospital Caen
 October 15 2020 Phase 1
NCT03643952 Completed
Bacteremia|Soft Tissue Infections|Skin Diseases Infectious
Merck Sharp & Dohme LLC
 December 6 2018 Phase 2

Chemical Information & Solubility

Molecular Weight 1620.67 Formula

C72H101N17O26
CAS No. 103060-53-3 SDF Download Daptomycin SDF
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
Storage (From the date of receipt)

In vitro
Batch:

Water : 100 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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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.

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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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