Daptomycin [103060-53-3]

Cat# HY-B0108-100mg

Size : 100mg

Brand : MedChemExpress

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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.

Solvent & Solubility
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
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.

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.

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)

g

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).
Purity & Documentation
References

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