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达托霉素 /Daptomycin {[allProObj[0].p_purity_real_show]}

货号:A520357 同义名: LY146032

Daptomycin is a lipopeptide antimicrobial agent with activity against Gram-positive organisms, including multi-resistant strains.

Daptomycin 化学结构 CAS号:103060-53-3
Daptomycin 化学结构
CAS号:103060-53-3
Daptomycin 3D分子结构
CAS号:103060-53-3
Daptomycin 化学结构 CAS号:103060-53-3
Daptomycin 3D分子结构 CAS号:103060-53-3
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Daptomycin 纯度/质量文件 产品仅供科研

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产品名称 DNA synthesis helicase RdRp ribonucleotide reductase tRNA synthetase YB-1 其他靶点 纯度
Fexinidazole 98%
Daptomycin 98%
Blasticidin S·HCl 98%
Metronidazole 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Triglycidyl isocyanurate p53 98+%
Nedaplatin 99%+
Bendamustine 98+%
Trifluridine 98%
Robinetin 99%+
Carboplatin 99%
Cidofovir 99%
Cisplatin 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

99%+
Oxaliplatin 98%
YK-4-279 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

99%+
RK-33 98%
Brr2-IN-3 99%+
Phen-DC3 Trifluoromethanesulfonate 98%
Favipiravir 97%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

97%
Didox 98%
(E)-3-AP 97%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, Kd: 42.1 nM

Leucyl-tRNA synthetase, IC50: 46.11 nM

98%
SU056 +

YB-1, IC50: 1.73 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Daptomycin 生物活性

靶点
  • DNA synthesis

描述 Daptomycin exhibits strong in vitro inhibitory and bactericidal activity against a range of bacterial strains. It is notably effective against nafcillin-susceptible and resistant staphylococci with a MIC90 (minimum inhibitory concentration for 90% of organisms) of ≤0.5 mg/L, and against enterococci with a MIC90 of ≤2.0 mg/L. Daptomycin demonstrates greater efficacy than vancomycin against most isolates tested. It stands out as the most potent agent against nafcillin-resistant staphylococci and ranks among the most effective treatments for enterococci, excluding trimethoprim-sulfamethoxazole. Notably, both daptomycin and vancomycin exhibit an increase in MIC when the bacterial inoculum is increased from 105 to 107 nM cfu/mL, suggesting a dose-dependent response to larger bacterial populations[1]. Daptomycin's efficacy is contained within a relatively narrow concentration range, from 0.125 to 2.0 mg/mL, showing higher activity compared to other agents tested against S. faecalis [2]. Additionally, daptomycin has been found to inhibit the formation of nucleotide-linked intermediates in bacterial biosynthetic processes[3].
体内研究

In vivo, daptomycin administered at 10 mg/kg twice daily significantly reduces bacterial load in the kidneys of infected models within 48 hours of starting treatment. When the dose is increased to 20 mg/kg and administered once daily, it becomes less effective initially but still significantly reduces bacterial colonies after four days of treatment. The efficacy of this regimen is comparable to that of vancomycin or combined vancomycin-gentamicin therapy administered twice daily[2].

体外研究

Daptomycin exhibits strong in vitro inhibitory and bactericidal activity against a range of bacterial strains. It is notably effective against nafcillin-susceptible and resistant staphylococci with a MIC90 (minimum inhibitory concentration for 90% of organisms) of ≤0.5 mg/L, and against enterococci with a MIC90 of ≤2.0 mg/L. Daptomycin demonstrates greater efficacy than vancomycin against most isolates tested. It stands out as the most potent agent against nafcillin-resistant staphylococci and ranks among the most effective treatments for enterococci, excluding trimethoprim-sulfamethoxazole. Notably, both daptomycin and vancomycin exhibit an increase in MIC when the bacterial inoculum is increased from 105 to 107 nM cfu/mL, suggesting a dose-dependent response to larger bacterial populations[1].

Daptomycin's efficacy is contained within a relatively narrow concentration range, from 0.125 to 2.0 mg/mL, showing higher activity compared to other agents tested against S. faecalis [2].

Additionally, daptomycin has been found to inhibit the formation of nucleotide-linked intermediates in bacterial biosynthetic processes[3].

Daptomycin 参考文献

[1]Benson CA, et al. Comparative in-vitro activity of LY146032 a new peptolide, with vancomycin and eight other agents against gram-positive organisms. J Antimicrob Chemother. 1987 Aug;20(2):191-6.

[2]Miniter PM, et al. Activity of LY146032 in vitro and in experimental enterococcal pyelonephritis. Antimicrob Agents Chemother. 1987 Aug;31(8):1199-203.

[3]Allen NE, et al. Inhibition of peptidoglycan biosynthesis in gram-positive bacteria by LY146032. Antimicrob Agents Chemother. 1987 Jul;31(7):1093-9.

Daptomycin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.62mL

0.12mL

0.06mL

3.09mL

0.62mL

0.31mL

6.17mL

1.23mL

0.62mL

Daptomycin 技术信息

CAS号103060-53-3
分子式C72H101N17O26
分子量 1620.67
别名 LY146032
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(64.79 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(61.7 mM),配合低频超声助溶

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