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Daptomycin Antibiotics for Mammalian Cell Culture inhibitor

Name: Daptomycin
SKU: S1373
Availability: InStock
Rating: 5 (23 reviews)

Cat.No.S1373

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

Chemical Structure

Molecular Weight: 1620.67

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.97%

99.97

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
THP-1	Antibacterial assay				Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level after 24 hrs in presence of thymidine	19188393
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	1620.67	Formula	C₇₂H₁₀₁N₁₇O₂₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	103060-53-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LY146032			Smiles	CCCCCCCCCC(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)O)C(=O)NC3C(OC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC3=O)CCCN)CC(=O)O)C)CC(=O)O)CO)C(C)CC(=O)O)CC(=O)C4=CC=CC=C4N)C

Solubility

In vitro
Batch:

Water : 100 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (3.09mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.830mg/ml (0.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	DNA synthesis ^[1] (Cell-free assay)
In vitro	Daptomycin (5 μg/ml) reduces cell viability by >99% and membrane potential by >90% within 30 min in Staphylococcus aureus. This compound exhibits rapid in vitro bactericidal activity against clinically significant strains of gram-positive pathogens including hemolytic streptococci, methicillin-resistant Staphylococcus aureus, and vancomycin-resistant enterococci. It acts at the cytoplasmic membrane of susceptible bacteria (8), as demonstrated by binding and fractionation studies. This agent also differs from that of some antimicrobial peptides (e.g., human neutrophil peptide 1) that are capable of rapid depolarization of the cytoplasmic membrane but do not induce cell death for 1 hour to 2 hours. It inserts into the cytoplasmic membrane of bacteria, as indicated by whole-cell and artificial membrane studies. ^[1] This compound demonstrates greater bactericidal activity than all other drugs tested, killing ≥3 log CFU/ml by 8 hours. It is a cyclic polypeptide derived from Streptomyces roseosporus and representing a class of antimicrobial agents known as the peptolides (acid lipopeptide antibiotics). It is also active against vancomycin-resistant gram-positive bacteria, including enterococci. This chemical is highly protein bound (94%), and its in vitro activity is altered in the presence of serum or albumin.^[2] It consists of a 13-member amino acid cyclic lipopeptide with a decanoyl side-chain, the lipophilic tail into the bacterial cell membrane, causing rapid membrane depolarization and a potassium ion efflux. Its treatment has been linked to fully reversible skeletal muscle toxicity with no effect on smooth or cardiac muscle. ^[3]
In vivo	Daptomycin exhibited linear pharmacokinetics, with an area under the concentration-time curve (AUC) from time zero to infinity/dose of 9.4 and a half-life of 0.9 to 1.4 h. The level of protein binding was 90%^[5].
References	[1] https://pubmed.ncbi.nlm.nih.gov/12878516/ [2] https://pubmed.ncbi.nlm.nih.gov/10722513/ [3] https://pubmed.ncbi.nlm.nih.gov/15705644/ [4] https://pubmed.ncbi.nlm.nih.gov/11181370/ [5] https://pubmed.ncbi.nlm.nih.gov/14693519/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04277143	Unknown status	Outcome Fatal\|Infection	Zhongnan Hospital	December 1 2020	--
NCT04434300	Completed	Antibiotics\|Subcutaneous Injection\|Daptomycin	University Hospital Caen	October 15 2020	Phase 1
NCT03643952	Completed	Bacteremia\|Soft Tissue Infections\|Skin Diseases Infectious	Merck Sharp & Dohme LLC	December 6 2018	Phase 2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Could you tell me the native source for this compound?

Answer:
It was synthesed from S.reseosporus.

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