Daptomycin

製品コードS1373 バッチS137308

化学情報

	Synonyms	LY146032	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₇₂H₁₀₁N₁₇O₂₆
	分子量	1620.67	CAS No.	103060-53-3
Solubility (25°C)*	体外	Water	100 mg/mL warmed with 50ºC water bath (61.7 mM)
		DMSO	Insoluble
		Ethanol	Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

動物実験	動物モデル	ICR/Swiss mice
	投薬量	0, 1, 2.5, 5, 10, 15, or 20 mg/kg
	投与方法	i.p.

参考

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カスタマーフィードバック

: 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の高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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