Micafungin sodium是抗真菌剂，抑制1, 3-beta-D-glucan的合成。

Micafungin Sodium is the sodium salt form of micafungin, a semi-synthetic echinocandin derived from a natural product of the fungus Coleophoma empetri with antifungal activity.

Micafungin (10 mg/mL) phenotypicly decreases the formation of biofilm in most of the isolates. The levels of mRNA transcription are also decreased significantly in micafungin-treated samples for all the genes tested, cf. their untreated counterparts[1]. The combination of micafungin and KB425796-C is fungicidal and markedly reduces the number of CFU, in contrast to the fungistatic effects (no reduction in CFU) observed at all examined time points when each drug is used alone[2].

Micafungin (1 mg/kg) significantly prolongs survival compared with mice administered saline. Animals given a combination of micafungin (0.1 mg/kg) and KB425796-C (32 mg/kg) show a trend towards prolonged survival in comparison with those treated with micafungin (0.1 mg/kg) alone. The number of CFUs decreases in the livers of micafungin-treated mice, despite the clearance effect being less than that found in the kidneys. Combination treatment with micafungin and KB425796-C results in a significant decrease in the number of CFUs compared with the treatment with micafungin alone at all examined doses. The clearance effect associated with KB425796-C in combination with micafungin is greater than that observed in AMPH-treated animals[2].

HEK-GPR119 cells are transfected with GloSensor 22F plasmid and used for dynamic cAMP measurements 24-30 h later. Cell suspensions are made by dislodging the cells using PBS wash and Accutase treatment followed by resuspension in culture media. Cells are then washed twice by pelleting through centrifugation (300 g, 5 min) and resuspension in assay buffer (Hank's Balanced Salt Solution supplemented with 20 mM HEPES and 0.01% fatty acid free BSA, pH 7.4). Cells are then counted and diluted to 600,000 cells/mL in buffer, before GloSensor cAMP reagent is added (2% v/v) and equilibrated with the cells for 2 h at 20°C with periodic mixing. 50 μl/well of cells are added to white-bottomed 384 well plates (30,000 cells/well) in triplicate and baseline luminescence is measuring using an Envision plate-reader. 5 μL of MBX-2982 (serially diluted in DMSO and then diluted 1:100 in assay buffer to obtain ×10 concentrated solution) is manually added to the assay wells to achieve the stated final concentration. Plates are incubated at 20°C with luminescence read at regular intervals to detect dynamic cAMP changes over time within the same wells. cAMP responses at each time-point are expressed as fold over control (vehicle-treated cells)[1].

Each fungal isolate is incubated statically in yeast-maltose (YM) agar broth for 24?h at 30°C.?Cryptococcus neoformans?YC203 is grown in YM broth medium for 20?h at 30°C with shaking at 200?r.p.m. A cell suspension is prepared by washing the cultured cells once with sterile saline.?A. fumigatus?FP1305 is cultured on a potato dextrose agar (PDA) slant for 4 days, and spores are then harvested in sterile saline and collected by filtering through gauze. Antifungal activity against all isolates, with the exception of C. neoformans, is measured by the micro-broth dilution method in 96-well culture plates using RPMI 1640 medium supplemented with?l-glutamine, but without sodium bicarbonate, and buffered to pH 7.0 with 0.165?m?MOPS. ForC. neoformans, yeast nitrogen base-glucose (YNBD) medium is used. For the assay, the test microorganism is inoculated into each well to yield 1×105?CFU/well, and the plates are then incubated for 20?h or 48?h at 37°C. Two end points are determined by microscopic observation: MEC, which is defined as a substantial reduction in fungal growth, and MIC, which is defined as a complete inhibition of growth.

208538-73-2

C56H70N9NaO23S

1292.27

Mycamine Sodium;FK 463;米卡芬净钠;FK463 Sodium

H2O:100 mg/mL (77.38 mM)
Ethanol:<1 mgml
DMSO:32 mg/mL(24.8 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years