Caspofungin (MK-0991) Acetate

Synonyms: L-743872

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

Caspofungin (MK-0991) Acetate Chemical Structure

Caspofungin (MK-0991) Acetate Chemical Structure

CAS No. 179463-17-3

Purity & Quality Control

Caspofungin (MK-0991) Acetate Related Products

Biological Activity

Description Caspofungin Acetate (MK-0991, L-743872) is an lipopeptide antifungal β-1,3-glucan synthase inhibitor.
Targets
β-1,3-glucan synthase [3]
In vitro
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)

Cell Research Cell lines Vero cells
Concentrations 20.78 μM
Incubation Time 2-3 days
Method

Vero cells were treated with the indicated concentrations of drugs for 2- or 3-days incubation

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

Chemical Information & Solubility

Molecular Weight 1213.42 Formula

C52H88N10O15.2C2H4O2

CAS No. 179463-17-3 SDF Download Caspofungin (MK-0991) Acetate SDF
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
Storage (From the date of receipt) 3 years -20°C(in the dark) powder

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


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In vivo
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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
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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