Reagentia en instrumenten voor immunologie, celbiologie en moleculaire biologie.

Daptomycin [103060-53-3]

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Referentie HY-B0108-50mg

Formaat : 50mg

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

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Synthèse de peptides personnalisée

Daptomycin Chemical Structure

CAS No. : 103060-53-3

This product is a controlled substance and not for sale in your territory.

Based on 16 publication(s) in Google Scholar

Other Forms of Daptomycin:

Daptomycin (Standard) Obtenir un devis

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

Description

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

IC₅₀ & Target

Lipopeptide

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]

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].

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

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].

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

Essai clinique

Masse moléculaire

1620.67

Formule

C₇₂H₁₀₁N₁₇O₂₆

CAS No.

103060-53-3

Appearance

Solid

Color

Off-white to light yellow

Structure Classification

Antibiotics
Disease Research
Antibacterial

Antibiotics
Macrolide Antibiotics

Antibiotics
Mammalian Cell Culture

Initial Source

Microorganisms

soil actinomycete

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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)

Solvant et solubilité

In Vitro:

H₂O : 100 mg/mL (61.70 mM; Need ultrasonic)

DMSO : ≥ 100 mg/mL (61.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculateur de molarité
Calculateur de dilution

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (1.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (1.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (1.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (61.70 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Pureté et documentation

Purity: 99.90%

Select Batch:

SDS (394 KB)

COA (248 KB) LCMS (99 KB)

Instruction de manipulation (2659 KB)

Références

[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]

Administration animale ^[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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références	[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]

Administration animale
^[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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

Références

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Daptomycin Related Classifications

Peptides
Peptide and Derivatives
Antimicrobial Peptides

Infection Cancer
Cancer Targeted Therapy Cancer Immunotherapy Cancer Drug Resistance

Anti-infection
Bacterial Antibiotic

Daptomycin [103060-53-3]

Referentie HY-B0108-50mg

Neem contact op met een lokale distributeur :

Merk : MedChemExpress

Neem contact op met een lokale distributeur :

Other Forms of Daptomycin:

Voir tous les produits spécifiques à Isoform Antibiotic:

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Daptomycin Related Classifications

Keywords:

Misschien heeft u ook interesse in de volgende producten:

Daptomycin [103060-53-3]

Referentie HY-B0108-50mg

Neem contact op met een lokale distributeur :

Merk : MedChemExpress

Neem contact op met een lokale distributeur :

Other Forms of Daptomycin:

Voir tous les produits spécifiques à Isoform Antibiotic:

Daptomycin Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Daptomycin Related Classifications

Keywords:

Misschien heeft u ook interesse in de volgende producten: