Daptomycin (Synonyms: 達(dá)托霉素; LY146032)

目錄號(hào): HY-B0108 純度: 99.90%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Daptomycin 是一種脂肽類抗生素，具有體外快速殺除革蘭氏陽(yáng)性細(xì)菌的活性。

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Custom Peptide Synthesis

Daptomycin Chemical Structure

CAS No. : 103060-53-3

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規(guī)格	價(jià)格	是否有貨
5 mg	￥213	In-stock
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

MCE 顧客使用本產(chǎn)品發(fā)表的 16 篇科研文獻(xiàn)

•Emerg Microbes Infect. 2024 Dec;13(1):2321981. [Abstract]
•Virulence. 2024 Oct 10:2415952. [Abstract]
•ACS Infect Dis. 2024 Jul 27. [Abstract]
•ACS Infect Dis. 2023 Nov 28. [Abstract]
•Appl Microbiol Biotechnol. 2022 Apr;106(7):2689-2702. [Abstract]
•iScience. 5 January 2022, 103731.
•Antimicrob Agents Chemother. 2021 Jan 20;65(2):e01275-20. [Abstract]
•Int J Med Microbiol. 2020 Jan;69(1):120-131. [Abstract]
•Pol J Microbiol. 2023 Jun 14;72(2):199-208. [Abstract]
•ACS Omega. 2023 Feb 2; 8 (6), 5415-5425.
•ACS Omega. March 3, 2022.
•Infect Drug Resist. 2021 Dec 16;14:5449-5456. [Abstract]

•Diagn Micr Infec Dis. 2020 Jul;97(3):115040. [Abstract]
•PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. [Abstract]
•bioRxiv. 2024 May 10.
•bioRxiv. 2023 Oct 2.

Daptomycin 相關(guān)產(chǎn)品

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

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

IC₅₀ & Target

Lipopeptide

細(xì)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]

體外研究
(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.

體內(nèi)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 號(hào)

103060-53-3

性狀

固體

顏色

Off-white to light yellow

中文名稱

達(dá)托霉素

結(jié)構(gòu)分類

初始來(lái)源

微生物

soil actinomycete

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : ≥ 100 mg/mL (61.70 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

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

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

摩爾計(jì)算器
稀釋計(jì)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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (1.28 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (1.28 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (1.28 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

方案一

請(qǐng)依序添加每種溶劑： PBS
Solubility: 100 mg/mL (61.70 mM); 澄清溶液; 超聲助溶

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

純度 & 產(chǎn)品資料

純度: 99.90%

選擇批次：

Data Sheet (628 KB) SDS (394 KB)

COA (286 KB) LCMS (99 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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.
參考文獻(xiàn)	[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.

參考文獻(xiàn)

[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 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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達(dá)托霉素LY 146032LY-146032BacterialAntibioticInhibitorinhibitorinhibit

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Daptomycin (Synonyms: 達(dá)托霉素; LY146032)

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