B2083-5mg | Caspofungin Acetate [179463-17-3] Clinisciences

Background

Caspofungin acetate (MK-0991), a new antifungal agent with minimal toxicity, inhibits synthesis of 1,3-β-D-glucan, an essential component of the fungal cell wall [1].

In vitro: Incubation of A. fumigatu with 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 within A. fumigateshyphae are killed when they are exposed to caspofungin [1]. 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 [2]. Caspofungin showed activity against Aspergillusspp. as well as a variety of Candidaspp[3]. 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) [4].

Clinical trials: In a trial of 128 patients with Candida esophagitis, clinical response rates were higher with caspofungin acetate 50 or 70 mg/day (85%) than with amphotericin B 0.5 mg/kg/day (67%) [2].

References:
[1] Bowman J C, Hicks P S, Kurtz M B, et al. The antifungal echinocandincaspofungin acetate kills growing cells of Aspergillus fumigatus in vitro [J]. Antimicrobial agents and chemotherapy, 2002, 46 (9): 3001-3012.
[2] Hoang A. Caspofungin acetate: an antifungal agent [J]. American journal of health-system pharmacy, 2001, 58 (13): 1206-1214.
[3] Pacetti S A, Gelone S P. Caspofungin acetate for treatment of invasive fungal infections [J]. Annals of Pharmacotherapy, 2003, 37 (1): 90-98.
[4] Bartizal K, Gill C J, Abruzzo G K, et al. In vitro preclinical evaluation studies with the echinocandin antifungal MK-0991 (L-743,872) [J]. Antimicrobial Agents and Chemotherapy, 1997, 41 (11): 2326-2332.

Product Citation

1. Granger BL. "Accessibility and contribution to glucan masking of natural and genetically tagged versions of yeast wall protein 1 of Candida albicans." PLoS One. 2018 Jan 12; 13 (1): e0191194. PMID:29329339

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	1213.42
Cas No.	179463-17-3
Formula	C₅₆H₉₆N₁₀O₁₉
Solubility	≥60.67 mg/mL in DMSO; insoluble in EtOH; ≥21.5 mg/mL in H2O
Chemical Name	acetic acid compound with (Z)-N-((2R,6S,7Z,9S,11R,12S,13E,14aS,15S,20S,21Z,23S,24Z,25aS)-20-((R)-3-amino-1-hydroxypropyl)-12-((2-aminoethyl)amino)-23-((1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl)-2,8,11,14,15,22,25-heptahydroxy-6-((R)-1-hydroxyethyl)-5
SDF	Download SDF
Canonical 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
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:
Cell lines	Aspergillus fumigates
Preparation method	The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.
Reacting condition	32 μg/mL for 6 h; or 2 μg/mL for 12 h
Applications	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.
References: 1 Walker, L. A., Lee, K. K., Munro, C. A. and Gow, N. A. (2015) Caspofungin Treatment of Aspergillus fumigatus Results in ChsG-Dependent Upregulation of Chitin Synthesis and the Formation of Chitin-Rich Microcolonies. Antimicrob Agents Chemother. 59, 5932-5941

Quality Control

Chemical structure

Caspofungin Acetate [179463-17-3]

Referentie B2083-5mg

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