Daptomycin (Synonyms: LY146032) |
| カタログ番号GC10214 |
ダプトマイシンは、グラム陽性菌に対する迅速な in vitro 殺菌活性を持つリポペプチド抗生物質です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 103060-53-3
Sample solution is provided at 25 µL, 10mM.
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Daptomycin is a lipopeptide antibiotic with rapid bactericidal activity against Gram-positive bacteria [1]. Daptomycin has in vitro activity against enterococci, staphylococci, streptococci, corynebacteria, and stationary-phase persistent bacteria Borrelia burgdorferi [2]. The antibacterial mechanism of daptomycin is different from that of most antibiotics. It uses acylglycerol phosphate to insert into the cell membrane and agglomerate, change the curvature of the cell membrane and perforate it, thereby triggering cell depolarization and leading to cell necrosis [3].
In vitro, Daptomycin(5μg/ml) reduces Staphylococcus aureus cell viability by >99% and membrane potential by >90% within 30 minutes[4]. Daptomycin (100 μg/ml) treated high-density exponentially growing Staphylococcus aureus ATCC 29213 cells for 60 minutes and had a very rapid bactericidal effect, reducing the number of bacteria by 3 logs[5].
In vivo, Daptomycin (20 mg/kg; i.p.) significantly improved the survival rate and reduced the number of viable bacteria and the level of neutrophil chemotactic factor KC in the peritoneal fluid 6h after treatment of peritonitis mice inoculated with enterococci.[6]. Daptomycin (60 mg/kg; s.c.) has moderate efficacy in the treatment of Staphylococcus aureus osteomyelitis in Sprague-Dawley CD rats [7].
References:
[1]Steenbergen J N , Jeff A , Thorne G M ,et al.Daptomycin: a lipopeptide antibiotic for the treatment of serious Gram-positive infections[J].Journal of Antimicrobial Chemotherapy2005(3):283-8.
[2] Feng J, Weitner M, Shi W, et al. Eradication of Biofilm-Like Microcolony Structures of Borrelia burgdorferi by Daunomycin and Daptomycin but not Mitomycin C in Combination with Doxycycline and Cefuroxime[J].Frontiers in Microbiology. 2016, 7: 62.
[3] Pogliano J, Pogliano N, Silverman JA. Daptomycin-mediated reorganization of membrane architecture causes mislocalization of essential cell division proteins. Journal of Bacteriology[J].September 2012, 194 (17): 4494–504.
[4] Silverman, Jared A, Perlmutter, et al. Correlation of Daptomycin Bactericidal Activity and Membrane Depolarization in Staphylococcus aureus[J].Antimicrob Agents Chemother. 2003 Aug;47(8):2538-44.
[5] Mascio C T M , Alder J D , Silverman J A. Bactericidal action of daptomycin against stationary-phase and nondividing Staphylococcus aureus cells[J]. Antimicrobial Agents and Chemotherapy, 2007, 51(12): 4255-4260.
[6]Kajihara T1, Nakamura S2, Iwanaga N3, et al. Comparative efficacies of daptomycin, vancomycin, and linezolid in experimental enterococcal peritonitis. J Infect Chemother. 2017 Jul;23(7):498-501.
[7]Poeppl W , Tobudic S , Lingscheid T ,et al. Daptomycin, Fosfomycin, or Both for Treatment of Methicillin-Resistant Staphylococcus aureus Osteomyelitis in an Experimental Rat Model[J].Antimicrobial Agents and Chemotherapy, 2011, 55(11):4999-5003.
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Cell experiment [1]: |
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Cell lines |
Methicillin-sensitive S. aureus strain ATCC 29213 |
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Preparation method |
over the 24h experiment, high cell density stationary-phase cultures of S. aureus in MHBc were treated with various concentrations of daptomycin (0, 8, 16, 32, 64, and 128 μg/ml). On the basis of the data generated from the concentration range-finding study, the bactericidal actions of daptomycin and comparator antibiotics were evaluated. |
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Reaction Conditions |
0, 8, 16, 32, 64, and 128 μg/ml; 24h |
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Applications |
The lower daptomycin concentration had a minimal effect on high inoculum density stationary-phase S. aureus over the 24-h experiment. Daptomycin concentration (100 μg/ml) had a very rapid bactericidal effect on high-density exponentially growing cells. |
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Animal experiment [2]: |
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Animal models |
Sprague-Dawley CD rats |
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Preparation method |
Sprague-Dawley CD rats with radiographically confirmed osteomyelitis of the tibia were randomly assigned to one of the following four treatment groups: (i) Daptomycin alone, (ii) FOF alone, (iii) the two drugs in combination, and (iv) saline placebo. Daptomycin powder was dissolved in sterile water and administered subcutaneously at a dose of 60 mg/kg of body weight once daily. |
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Dosage form |
60mg/kg; s.c. |
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Applications |
Daptomycin has only modest benefit in treating osteomyelitis. |
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References: [1] Mascio C T M , Alder J D , Silverman J A. Bactericidal action of daptomycin against stationary-phase and nondividing Staphylococcus aureus cells[J]. Antimicrobial Agents and Chemotherapy, 2007, 51(12): 4255-4260. [2] Poeppl W , Tobudic S , Lingscheid T ,et al.Daptomycin, Fosfomycin, or Both for Treatment of Methicillin-Resistant Staphylococcus aureus Osteomyelitis in an Experimental Rat Model[J].Antimicrobial Agents and Chemotherapy, 2011, 55(11):4999-5003. |
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| Cas No. | 103060-53-3 | SDF | |
| 同義語 | LY146032 | ||
| Canonical 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 | ||
| Formula | C72H101N17O26 | M.Wt | 1620.67 |
| 溶解度 | ≥ 81.05mg/mL in DMSO or Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.617 mL | 3.0851 mL | 6.1703 mL |
| 5 mM | 0.1234 mL | 0.617 mL | 1.2341 mL |
| 10 mM | 0.0617 mL | 0.3085 mL | 0.617 mL |
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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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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