Daptomycin
(Synonyms: 达托霉素; LY146032) 目录号 : GC10214
达托霉素（Daptomycin）是一种脂肽抗生素，对革兰氏阳性菌具有快速的杀菌活性。
Cas No.:103060-53-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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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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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.
达托霉素（Daptomycin）是一种脂肽抗生素，对革兰氏阳性菌具有快速的杀菌活性[1]。达托霉素对肠球菌、葡萄球菌、链球菌、棒状杆菌和静止期伯氏疏螺旋体持留细菌具有体外活性[2]。达托霉素的抑菌作用机制与大多数抗生素不同，是利用磷酸酰甘油让其插入细胞膜中，并且凝集，改变细胞膜的曲度并穿孔，进而引发细胞去极化导致细胞坏死[3]。
在体外，达托霉素（5 μg/ml）在30分钟内能够降低金黄色葡萄球菌>99%的细胞活性和>90%的膜电位[4]。达托霉素（100μg/ml）处理高密度指数生长的金黄色葡萄球菌ATCC 29213细胞60分钟，具有非常快速的杀菌作用，减少了3个对数的细菌数量[5]。
在体内，达托霉素（20mg/kg; i.p.）治疗接种肠球菌后的腹膜炎小鼠6h后，显著提高了存活率，降低了腹腔液中活菌数量和中性粒细胞趋化因子KC水平[6]。达托霉素（60mg/kg; s.c.）治疗Sprague-Dawley CD大鼠金黄色葡萄球菌骨髓炎的效果一般[7]。
| Cas No. | 103060-53-3 | SDF | |
| 别名 | 达托霉素; 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 | ||
| 分子式 | C72H101N17O26 | 分子量 | 1620.67 |
| 溶解度 | ≥ 81.05mg/mL in DMSO or Water | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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