Daptomycin is a lipopeptide antimicrobial agent with activity against Gram-positive organisms, including multi-resistant strains.
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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。 |
靶点 |
|
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]. |
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 |
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 |
动物实验配方 |