research use only
Cat.No.S1373
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase |
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| Other Antibiotics for Mammalian Cell Culture Inhibitors | Tylosin tartrate |
| 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 | |||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
Water : 100 mg/mL
DMSO
: Insoluble
Ethanol : Insoluble |
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In vivo |
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| Molecular Weight | 1620.67 | Formula | C72H101N17O26 |
Storage (From the date of receipt) | |
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| CAS No. | 103060-53-3 | Download SDF | Storage of Stock Solutions |
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| Synonyms | LY146032 | 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 | ||
| Targets/IC50/Ki |
DNA synthesis
(Cell-free assay) |
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| In vitro |
Daptomycin (5 μg/ml) reduces cell viability by >99% and membrane potential by >90% within 30 min in Staphylococcus aureus. This compound 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. It acts at the cytoplasmic membrane of susceptible bacteria (8), as demonstrated by binding and fractionation studies. This agent 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. It inserts into the cytoplasmic membrane of bacteria, as indicated by whole-cell and artificial membrane studies. This compound demonstrates greater bactericidal activity than all other drugs tested, killing ≥3 log CFU/ml by 8 hours. It is a cyclic polypeptide derived from Streptomyces roseosporus and representing a class of antimicrobial agents known as the peptolides (acid lipopeptide antibiotics). It is also active against vancomycin-resistant gram-positive bacteria, including enterococci. This chemical is highly protein bound (94%), and its in vitro activity is altered in the presence of serum or albumin. It consists of a 13-member amino acid cyclic lipopeptide with a decanoyl side-chain, the lipophilic tail into the bacterial cell membrane, causing rapid membrane depolarization and a potassium ion efflux. Its treatment has been linked to fully reversible skeletal muscle toxicity with no effect on smooth or cardiac muscle. |
| 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%. |
References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| 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 |
Tel: +1-832-582-8158 Ext:3
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Question 1:
Could you tell me the native source for this compound?
Answer:
It was synthesed from S.reseosporus.