受注:045-509-1970 |
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Synonyms | LY146032 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C72H101N17O26 |
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分子量 | 1620.67 | CAS No. | 103060-53-3 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (61.7 mM) | ||||||||
Water (warmed with 50ºC water bath) | 50 mg/mL (30.85 mM) | ||||||||||
Ethanol | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | Daptomycin is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms. |
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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. 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]. |
動物実験 | 動物モデル | ICR/Swiss mice |
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投薬量 | 0, 1, 2.5, 5, 10, 15, or 20 mg/kg | |
投与方法 | i.p. |
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]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。