米卡芬净钠 T1794

Product Introduction
Bioactivity


英文名: Micafungin sodium

描述: Micafungin sodium (FK 463) 是抗真菌剂，抑制1, 3-beta-D-glucan 的合成。

细胞实验: 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.

激酶实验: 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].

体外活性: 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].

体内活性: 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].

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

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 45 mg/mL (34.82 mM)
H2O : 100 mg/mL (77.38 mM)


关键字: Inhibitor | Antibiotic | Fungal | inhibit | Micafungin | FK463 | FK-463 | Micafungin sodium

相关产品: WAY-604663 | Tylvalosin | Gatifloxacin hydrochloride | Tilmicosin | Nitrofurazone | Cefotaxime sodium | Gramicidin | Clioquinol | Carbadox | Artemether

相关库: Drug Repurposing Compound Library | Approved Drug Library | Antibiotics Library | FDA-Approved & Pharmacopeia Drug Library | Clinical Compound Library | Macrocyclic Compound Library | NMPA-Approved Drug Library | Anti-Fungal Compound Library | NO PAINS Compound Library | Anti-Infection Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途