product name Caspofungin Acetate
Description: Caspofungin acetate (also known as MK-0991) is a lipopeptide antifungal drug. It is a semi-synthetic analogue of pneumocandin B0 with improved water solubility, a significant limitation in the development of the echinocandin class as pharmaceuticals. Caspofungin acts by inhibition of the synthesis of β (1,3)-D-glucan, an essential component of the cell wall of susceptible fungi. Incubation ofA. fumigatuwith a single dose of caspofungin affected the same proportion of apical and subapical branching cells for up to 72 h.The cells at the active centers for new cell wall synthesis withinA. fumigateshyphae are killed when they are exposed to caspofungin.
References: Crit Care Med. 2003 May;31(5):1577-8; Antimicrob Agents Chemother. 1997 Nov;41(11):2326-32.
1213.42
Formula
C56H96N10O19
CAS No.
179463-17-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (82.4 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (82.4 mM)
Solubility (In vivo)
Synonyms
MK-0991
other peoduct :
| In Vitro |
In vitro activity: Incubation ofA. fumigatuwith a single dose of caspofungin affected the same proportion of apical and subapical branching cells for up to 72 h.The cells at the active centers for new cell wall synthesis withinA. fumigateshyphae are killed when they are exposed to caspofungin. Caspofungin acetate irreversibly inhibited the enzyme 1,3-β-D-glucan synthase, preventing the formation of glucan polymers and disrupting the integrity of the fungal cell wall. The elimination half-life of caspofungin acetate was 9-10 hours. Caspofungin showed activity againstAspergillusspp. as well as a variety ofCandidaspp. Growth kinetic studies of caspofungin acetate against Candida albicans and Candida tropicalis isolates showed that caspofungin acetate exhibited fungicidal activity (i.e., a 99% reduction in viability) within 3 to 7 h at concentrations ranging from 0.06 to 1 μg/ml (0.25 to 4 times the MIC)[4].The minimal inhibitory concentration for 90% inhibition of Candida species by caspofungin acetate were 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). Kinase Assay: Cell Assay: Caspofungin suppressed the synthesis of cell wall β-1,3-glucan, which triggered a compensatory stimulation of chitin synthesis. Caspofungin induced morphological changes in Aspergillus fumigates. Moreover, Treatment with caspofungin induced ChsG-dependent upregulation of chitin synthesis and the formation of chitin-rich microcolonies in Aspergillus fumigates. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Crit Care Med. 2003 May;31(5):1577-8; Antimicrob Agents Chemother. 1997 Nov;41(11):2326-32. |
