Daptomycin (Synonyms: 达托霉素; LY146032)

目录号: HY-B0108 纯度: 99.90%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Daptomycin 是一种脂肽类抗生素，具有体外快速杀除革兰氏阳性细菌的活性。

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Custom Peptide Synthesis

Daptomycin Chemical Structure

CAS No. : 103060-53-3

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规格	价格	是否有货
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10 mg	￥342	In-stock
25 mg	￥650	In-stock
50 mg	￥1100	In-stock
100 mg	￥1989	In-stock
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Customer Review

Other Forms of Daptomycin:

Daptomycin (Standard) 询价

MCE 顾客使用本产品发表的 16 篇科研文献

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Daptomycin is a lipopeptide antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.

IC₅₀ & Target

Lipopeptide

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HEK293	CC₅₀	> 100 μM Compound: Daptomycin	Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue reporter assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue reporter assay	[PMID: 30392371]
MDCK	EC₅₀	0.18 mg/L Compound: Daptomycin	Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in wild type MDCK cells after 24 hrs in presence of 100 uM verapamil Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in wild type MDCK cells after 24 hrs in presence of 100 uM verapamil	[PMID: 17548493]
MDCK	EC₅₀	0.62 mg/L Compound: Daptomycin	Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in wild type MDCK cells after 24 hrs Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in wild type MDCK cells after 24 hrs	[PMID: 17548493]
MDCK	EC₅₀	0.7 mg/L Compound: Daptomycin	Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in MDCK cells over expressing human MADR1 after 24 hrs in presence of 100 uM verapamil Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in MDCK cells over expressing human MADR1 after 24 hrs in presence of 100 uM verapamil	[PMID: 17548493]
MDCK	EC₅₀	2.67 mg/L Compound: Daptomycin	Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in MDCK cells over expressing human MADR1 at 1 mg/liter after 24 hrs Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in MDCK cells over expressing human MADR1 at 1 mg/liter after 24 hrs	[PMID: 17548493]
THP-1	EC₅₀	0.27 mg/L Compound: Daptomycin	Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in human THP1 cells after 24 hrs in presence of 0.5 uM elacridar Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in human THP1 cells after 24 hrs in presence of 0.5 uM elacridar	[PMID: 17548493]
THP-1	EC₅₀	0.31 mg/L Compound: Daptomycin	Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in human THP1 cells after 24 hrs in presence of 100 uM verapamil Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in human THP1 cells after 24 hrs in presence of 100 uM verapamil	[PMID: 17548493]
THP-1	EC₅₀	1.14 mg/L Compound: Daptomycin	Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in human THP1 cells after 24 hrs Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 phagocytized in human THP1 cells after 24 hrs	[PMID: 17548493]

体外研究
(In Vitro)

Daptomycin has excellent in-vitro inhibitory and bactericidal activity against nafcillin-susceptible and resistant staphylococci (MIC₉₀ less than or equal to 0.5 mg/L) and against enterococci (MIC₉₀ less than or equal to 2.0 mg/L). Daptomycin is more active than vancomycin against the majority of isolated tested. With the exception of trimethoprim-sulphamethoxazole, daptomycin is the most active agent in vitro against enterococci, and is the most active against nafcillin-resistant staphylococci. Daptomycin and vancomycin show a marked increase in MIC when the inoculum is increased from 10⁵ to 10⁷ cfu/mL^[1]. Daptomycin is effective within a very narrow range of drug concentrations (from 0.125 to 2.0 tLg/mL) and is more active than other agents tested against S. faecalis^[2]. Daptomycin inhibits the formation of these nucleotide-linked intermediates^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

At a dose of 10 mg/kg given twice daily, daptomycin reduces the number of organisms per kidney significantly compared with that in infected untreated controls within 48 h after the initiation of therapy. At 20 mg/kg given once a day, daptomycin is less effective but reduces colony counts significantly after 4 days of therapy, and its activity is comparable to that of vancomycin or vancomycin-gentamicin given twice daily^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

1620.67

Formula

C₇₂H₁₀₁N₁₇O₂₆

CAS 号

103060-53-3

性状

固体

颜色

Off-white to light yellow

中文名称

达托霉素

结构分类

初始来源

微生物

soil actinomycete

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-80°C	2 years
	-20°C	1 year
In solvent	-80°C	1 year
	-20°C	6 months

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (61.70 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : 100 mg/mL (61.70 mM; 超声助溶)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.6170 mL	3.0851 mL	6.1703 mL
5 mM	0.1234 mL	0.6170 mL	1.2341 mL
10 mM	0.0617 mL	0.3085 mL	0.6170 mL

查看完整储备液配制表

* 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, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (1.28 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (1.28 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (1.28 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (61.70 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.90%

选择批次：

Data Sheet (628 KB) SDS (394 KB)

COA (286 KB) LCMS (99 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

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

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

Animal Administration ^[2]	Inocula containing 109 CFU/mL are prepared from an 18-h brain heart infusion broth culture. The exact number in each inoculum is subsequently determined by the standard serial 10-fold dilution agar pour plate technique. Animals are challenged intravenously with a 1.0-mL inoculum. This inoculum is known to infect the renal medulla of normal rats. Twenty-four hours later the animals are divided into eight groups and are given either saline only (controls) or antibiotic therapy initiated with Daptomycin at 10 mg/kg (Daptomycin10), Daptomycin at 20 mg/kg (Daptomycin20), Daptomycin10 plus gentamicin at 1.5 mg/kg, vancomycin at 20 mg/kg, vancomycin at 20 mg/kg plus gentamicin at 1.5 mg/kg, ampicillin at 30 mg per rat per injection, and ampicillin at 30 mg per rat plus gentamicin at 1.5 mg/kg. Animals receive Daptomycin20 once daily; all other drugs are administered twice daily. Vancomycin and Daptomycin are given subcutaneously; ampicillin and gentamicin are given intramuscularly. Drugs are administered for up to 13 days. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [2]. Miniter PM, et al. Activity of LY146032 in vitro and in experimental enterococcal pyelonephritis. Antimicrob Agents Chemother. 1987 Aug;31(8):1199-203. [Content Brief] [3]. Allen NE, et al. Inhibition of peptidoglycan biosynthesis in gram-positive bacteria by LY146032. Antimicrob Agents Chemother. 1987 Jul;31(7):1093-9. [Content Brief]

Animal Administration
^[2]

Inocula containing 109 CFU/mL are prepared from an 18-h brain heart infusion broth culture. The exact number in each inoculum is subsequently determined by the standard serial 10-fold dilution agar pour plate technique. Animals are challenged intravenously with a 1.0-mL inoculum. This inoculum is known to infect the renal medulla of normal rats. Twenty-four hours later the animals are divided into eight groups and are given either saline only (controls) or antibiotic therapy initiated with Daptomycin at 10 mg/kg (Daptomycin10), Daptomycin at 20 mg/kg (Daptomycin20), Daptomycin10 plus gentamicin at 1.5 mg/kg, vancomycin at 20 mg/kg, vancomycin at 20 mg/kg plus gentamicin at 1.5 mg/kg, ampicillin at 30 mg per rat per injection, and ampicillin at 30 mg per rat plus gentamicin at 1.5 mg/kg. Animals receive Daptomycin20 once daily; all other drugs are administered twice daily. Vancomycin and Daptomycin are given subcutaneously; ampicillin and gentamicin are given intramuscularly. Drugs are administered for up to 13 days.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. [Content Brief]

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

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

Daptomycin 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	0.6170 mL	3.0851 mL	6.1703 mL	15.4257 mL
	5 mM	0.1234 mL	0.6170 mL	1.2341 mL	3.0851 mL
	10 mM	0.0617 mL	0.3085 mL	0.6170 mL	1.5426 mL
	15 mM	0.0411 mL	0.2057 mL	0.4114 mL	1.0284 mL
	20 mM	0.0309 mL	0.1543 mL	0.3085 mL	0.7713 mL
	25 mM	0.0247 mL	0.1234 mL	0.2468 mL	0.6170 mL
	30 mM	0.0206 mL	0.1028 mL	0.2057 mL	0.5142 mL
	40 mM	0.0154 mL	0.0771 mL	0.1543 mL	0.3856 mL
	50 mM	0.0123 mL	0.0617 mL	0.1234 mL	0.3085 mL
	60 mM	0.0103 mL	0.0514 mL	0.1028 mL	0.2571 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Daptomycin103060-53-3LY146032达托霉素LY 146032LY-146032BacterialAntibioticInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Daptomycin (Synonyms: 达托霉素; LY146032)

Customer Review

Other Forms of Daptomycin:

MCE 顾客使用本产品发表的 16 篇科研文献