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Caspofungin (MK-0991) Acetate Fungal inhibitor

Cat.No.S3073

Caspofungin Acetate (MK-0991, L-743872) is an lipopeptide antifungal β-1,3-glucan synthase inhibitor.
Caspofungin (MK-0991) Acetate Fungal inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 1213.42

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 1213.42 Formula

C52H88N10O15.2C2H4O2

Storage (From the date of receipt) 3 years -20°C(in the dark) powder
CAS No. 179463-17-3 Download SDF Storage of Stock Solutions

Synonyms L-743872 Smiles CCC(C)CC(C)CCCCCCCCC(=O)NC1CC(C(NC(=O)C2C(CCN2C(=O)C(NC(=O)C(NC(=O)C3CC(CN3C(=O)C(NC1=O)C(C)O)O)C(C(C4=CC=C(C=C4)O)O)O)C(CCN)O)O)NCCN)O.CC(=O)O.CC(=O)O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (82.41 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 50 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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
β-1,3-glucan synthase [3]
In vitro

Caspofungin acetate is the first in a new class of antifungals that inhibits the synthesis of beta (1, 3)-d-glucan, an essential component of the cell wall of filamentous fungi. Prior studies have shown in vitro activity of caspofungin acetate using the reference methods, broth microdilution or macrodilution, for antifungal susceptibility testing of Candida species established by the National Committee for Clinical Laboratory Standards 1997 guidelines against a variety of Candida species including Candida krusei. Although caspofungin acetate is only Food and Drug Administration-approved for the treatment of aspergillosis, there is information showing that many Candida species are susceptible. The minimal inhibitory concentration for 90% inhibition of Candida species by caspofungin acetate are as follows:C. albicans 0.5 μg/mL (range, 0.25-0.5), C. glabrata 1.0 μg/mL (range, 0.25-2.0), C. tropicalis 1.0 μg/mL (range, 0.25-1.0), C. parapsilosis 0.5 μg/mL (range, 0.25-1.0), and C. krusei 2.0 μg/mL (range, 0.5-2.0)

References
  • https://pubmed.ncbi.nlm.nih.gov/33917182/
  • https://pubmed.ncbi.nlm.nih.gov/21518846/

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04674657 Unknown status
Critical Illness|Extracorporeal Membrane Oxygenation Complication|Infection
Royal Brompton & Harefield NHS Foundation Trust
September 3 2018 --
NCT03399032 Completed
Septic Shock|Fungal Infection|Critical Illness
Medical University of Lublin
February 5 2018 --
NCT02805049 Completed
Septic Shock|Peritonitis
Centre Hospitalier Universitaire de Nīmes
January 28 2017 Phase 4
NCT03798600 Completed
Critical Illness|Infection
Careggi Hospital
January 1 2016 --
NCT02596984 Completed
Shock
Centre Hospitalier Universitaire de Saint Etienne|Merck Sharp & Dohme LLC
March 16 2015 Not Applicable

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