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Daptomycin

现货
Catalog No.
A1206
钙依赖抗生素
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
25mg
¥ 500.00
Ship with 10-15 days
100mg
¥ 1,800.00
Ship with 10-15 days

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Background

Daptomycin is a bactericidal antibiotic which works against a broad spectrum of Gram-positive bacteria and it can work both in-vitro and in-vivo. It is a cyclic lipopeptide and many antibiotic resistant strains can be inhibited by daptomycin, such as meticillin-resistant S. aureus (MRSA), vancomycin-intermediate S. aureus (VISA) and vancomycin-resistant S. aureus (VRSA).[1, 2]

The mode of action of Daptomycin would be through a calcium-dependent interaction with the cytoplasmic membrane, thus leading to the cell membrane depolarisation, ion loss and cell death.[2] Daptomycin can bind to the lipid tail of cell membrane of Gram-positive cells, then the following Ca2+ dependent insertion of daptomycin and oligomerization can cause a damage to the bacterial membrane potential, thus kills the cell very fast.[3]

References:
[1] Feng Wang, Ni-Ni Ren, Shuai Luo, Xiao-Xia Chen, Xu-Ming Mao, Yong-Quan Li. DptR2, a DeoR-type auto-regulator, is required for daptomycin production in Streptomyces roseosporus. Gene. 10 July 2014. 544(2): 208-215.
[2] Diixa Patel, Mashkur Husain, Celine Vidaillac, Molly E. Steed, Michael J. Rybak, Susan M. Seo, Glenn W. Kaatz. Mechanisms of in-vitro-selected daptomycin-non-susceptibility in Staphylococcus aureus. International Journal of Antimicrobial Agents. November 2011. 38(5): 442-446.
[3] Yong He, Jing Li, Nin Yin, Prudencio S. Herradura, Larry Martel, Yanzhi Zhang, Andre L. Pearson, Vidya Kulkarni, Carmela Mascio. Reduced pulmonary surfactant interaction of daptomycin analogs via tryptophan replacement with alternative amino acids. Bioorganic & Medicinal Chemistry Letters. 1 October 2012. 22(19): 6248-6251.

文献引用

1. Brennan-Krohn T, Pironti A, Kirby JE. "Synergistic Activity of Colistin-Containing Combinations against Colistin-Resistant Enterobacteriaceae."Antimicrob Agents Chemother. 2018 Jul 30. pii: AAC.00873-18. PMID:30061285

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt1620.67
Cas No.103060-53-3
FormulaC72H101N17O26
Solubility≥81.05mg/mL in DMSO or H2O
SDFDownload SDF
Canonical SMILESCCCCCCCCCC(=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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

甲氧西林易感金黄色葡萄球菌(ATCC#29213)

溶解方法

在DMSO中的溶解度>81.1mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

MIC: l μg/mL

应用

在甲氧西林易感金黄色葡萄球菌(ATCC#29213)中,Daptomycin (DAP) 在补充有50mg/L钙(MHBc)的Mueller-Hinton肉汤中对金黄色葡萄球菌保持良好的抗菌活性。

动物实验[2]:

动物模型

肠球菌实验性腹膜炎小鼠模型

剂量

50 mg/kg; q24h,静脉内给药(i.v.); 肠球菌接种后2小时,给药48小时

应用

在腹腔注射4×1010菌落形成单位的屎肠球菌小鼠中,Daptomycin(DAP)显著延长了直到死亡的平均时间。DAP或DAP加AMP显著降低接种后6 h腹膜液的活菌数。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1] Yong He, Jing Li, Nin Yin, Prudencio S. Herradura, Larry Martel, Yanzhi Zhang, Andre L. Pearson, Vidya Kulkarni, Carmela Mascio. Reduced pulmonary surfactant interaction of daptomycin analogs via tryptophan replacement with alternative amino acids. Bioorganic & Medicinal Chemistry Letters. 1 October 2012. 22(19): 6248-6251.

[2] 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.

质量控制

化学结构

Daptomycin

相关生物数据

Daptomycin

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Daptomycin