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Caspofungin Acetate

Catalog No. T1799   CAS 179463-17-3
Synonyms: L 743873, Cancidas, MK 0991, L 743872

Caspofungin Acetate (MK 0991) is the acetate salt of an antimycotic echinocandin lipopeptide, semisynthetically derived from a fermentation product of the fungus Glarea lozoyensis. This agent is active against Aspergillus and Candida species.

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Caspofungin Acetate Chemical Structure
Caspofungin Acetate, CAS 179463-17-3
Pack Size Availability Price/USD Quantity
5 mg In stock $ 52.00
10 mg In stock $ 77.00
25 mg In stock $ 157.00
50 mg In stock $ 283.00
100 mg In stock $ 441.00
1 mL * 10 mM (in DMSO) In stock $ 106.00
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Purity: 99.9%
Purity: 99.22%
Purity: 99.04%
Purity: 98.37%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Caspofungin Acetate (MK 0991) is the acetate salt of an antimycotic echinocandin lipopeptide, semisynthetically derived from a fermentation product of the fungus Glarea lozoyensis. This agent is active against Aspergillus and Candida species.
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)
In vivo Mice injected with caspofungin at vitreal concentrations from 0.41 to 4.1 μM cause no significant alterations in their ERG waveforms and their retinas have no detectable morphologic changes or loss of cells. At the vitreal concentration of 41 μM, caspofungin reduces the amplitudes of the a-waves, b-waves, and scotopic threshold responses of the ERG and also produces a decrease in the number of cells in the ganglion cell layer[4]. Caspofungin (8 mg/kg) or amphotericin B at 1 mg/kg given i.p. once daily for 7 days beginning at 30 h after infection resulted in 100% survival through day 28 relative to vehicle control treatment, which results in 100% mortality by day 11 after infectious challenge. Caspofungin reduces recovery of viable Candida from kidney and brain tissues compared to vehicle control treatment on day 5, when control burden peaked. Caspofungin-treated mice dosed with 2 mg/kg or greater have significantly lower brain burden than amphotericin-B-treated mice at day 5. Amphotericin B and caspofungin treatment reduce kidney fungal burden by 1.7 log CFU/g and 2.46 to 3.64 log CFU/g, respectively[5].
Synonyms L 743873, Cancidas, MK 0991, L 743872
Molecular Weight 1213.42
Formula C56H96N10O19
CAS No. 179463-17-3

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 83.3 mg/mL (68.65 mM)

H2O: 100 mg/mL (82.41 mM)

TargetMolReferences and Literature

1. McGee WT, et al. Crit Care Med, 2003, 31(5), 1577-1578. 2. Bartizal K, et al. Antimicrob Agents Chemother, 1997, 41(11), 2326-2332. 3. Leonard WR Jr, et al. J Org Chem. 2007, 72(7):2335-43. 4. Mojumder DK, et al. Evaluating retinal toxicity of intravitreal caspofungin in the mouse eye. Invest Ophthalmol Vis Sci. 2010 Nov;51(11):5796-803. 5. Flattery, Amy M. et al. Efficacy of caspofungin in a juvenile mouse model of central nervous system candidiasis. Antimicrobial Agents and Chemotherapy (2011), 55(7), 3491-3497. 6. Wang M, Ye F, Su J, et al. Caspofungin and LTX-315 inhibit SARS-CoV-2 replication by targeting the nsp12 polymerase[J]. 2020 7. Tsang C C, Tang J Y M, Ye H, et al. Rare/cryptic Aspergillus species infections and importance of antifungal susceptibility testing[J]. Mycoses. 2020, 63(12): 1283-1298. 8. Tsang C C, Chan K F, Chan W, et al. Hepatic phaeohyphomycosis due to a novel dematiaceous fungus, Pleurostoma hongkongense sp. nov., and importance of antifungal susceptibility testing[J]. Emerging Microbes & Infections. 2020: 1-53.

TargetMolCitations

1. Ma L, Lian Y, Tang J, et al. Identification of the Anti-Fungal Drug Fenticonazole Nitrate as a Novel PPARγ-Modulating Ligand With Good Therapeutic Index: Structure-Based Screening and Biological Validation. Pharmacological Research. 2021: 105860. 2. Quan C, Chen Y, Wang X, et al. Loss of histone lysine methyltransferase EZH2 confers resistance to tyrosine kinase inhibitors in non-small cell lung cancer. Cancer Letters. 2020 3. Tsang C C, Chan K F, Chan W, et al. Hepatic phaeohyphomycosis due to a novel dematiaceous fungus, Pleurostoma hongkongense sp. nov., and importance of antifungal susceptibility testing. Emerging Microbes & Infections. 2021 Dec;10(1):81-96.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Clinical Compound Library NO PAINS Compound Library FDA-Approved & Pharmacopeia Drug Library Approved Drug Library Anti-Fungal Compound Library Anti-Infection Compound Library Cyclic Peptide Library Macrocyclic Compound Library Antibiotics Library

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Keywords

Caspofungin Acetate 179463-17-3 Microbiology/Virology Antibiotic Antifungal fungal cell wall inhibit MK-0991 diacetate L743873 MK-0991 Fungal Inhibitor L-743872 antifungal L 743873 Caspofungin diacetate MK0991 L-743873 Cancidas L-743872 diacetate MK 0991 L743872 L 743872 inhibitor

 

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