Anidulafungin (Ecalta) (LY303366) is an echinocandin derivative used as an antifungal drug. It inhibits glucan synthase activity.

Anidulafungin（LY-303366）对所有测试的Candida albicans（n=99）、Candida glabrata（n=18）、Candida tropicalis（n=10）分离株的最低抑菌浓度（MIC）均≤0.32 μg/mL。Anidulafungin对Aspergillus种（90%分离株被抑制的最低有效浓度，0.02 μg/mL）亦有活性（n=20），但对Candida parapsilosis的活性较低（90%分离株被抑制的MIC [MIC90]，5.12 μg/mL）（n=10），对C. neoformans（MIC90 >10.24 μg/mL）（n=15）和B. dermatitidis（MIC90，16 μg/mL）（n=29）无活性。Fluconazole对三株C. tropicalis、七株C. glabrata和两株Candida krusei的MIC均≥16 μg/mL。对这12株中的11株，Anidulafungin的MIC范围从0.08至0.32 mg/mL。第十二株为C. krusei（Fluconazole MIC，32 μg/mL)，其Anidulafungin MIC为1.28 mg/mL。这12株的90%抑制MIC（MIC90）为0.32 μg/mL。对于Fluconazole MIC≥8 μg/mL的其余18株C. glabrata和C. tropicalis分离株，Anidulafungin的MIC90也是0.32 mg/mL。Anidulafungin对Fluconazole MIC ≥16 mg/mL的Candida种同对Fluconazole MIC ≥8 μg/mL的种表现出同等活性。与C. albicans、C. glabrata和C. tropicalis相比，Anidulafungin对C. neoformans和B. dermatitidis的活性显著较低。Ketoconazole和amphotericin B是对C. neoformans和B. dermatitidis测试中最活跃的抗真菌药。Anidulafungin对Aspergillus种展示出强大的体外活性，其MEC90为0.02 μg/mL。对照种酵母分离株的Anidulafungin MIC为C. albicans ATCC 90028的0.02 μg/mL，C. glabrata ATCC 90030的0.16 mg/mL，C. neoformans ATCC 90112的>10.24 μg/mL。通过CD101选择的菌株若CD101 MIC增加至少2倍，其Anidulafungin（ANF）和/或Caspofungin（CSF）的MIC也至少增加2倍。

FITC-S1P quantification/Caliper assay: A 384-well format of the SphK enzyme assay based on separation of FITC-S1P from unreacted FITC-sphingosine substrate using a microfluidic capillary electrophoresis mobility-shift system is developed. Briefly, 3 nM SphK1–His6 is incubated with 1 μM FITC-sphingosine, 20 μM ATP and 10 μM compound (a final concentration of DMSO of 2 %) in a buffer containing 100 mM Hepes (pH 7.4), 1 mM MgCl2,0.01% Triton X-100, 10% glycerol, 100 μM sodium orthovanadate and 1 mM DTT for 1 h in a 384-well Matrical MP-101-1-PP plate. Reaction mixtures (10 μL) are quenched by the addition of 20 μL of 30 mM EDTA and 0.15% Coating Reagent-3 in 100 mM Hepes, and a small aliquot of each reaction (a few nanolitres) is analysed in the Caliper LabChip 3000 instrument under -1.5 psi (psi=6.9 kPa) pressure, a downstream voltage of -1900 V and a sip time of 0.2 s. Phosphorylated fluorescent product and unphosphorylated fluorescent substrate appeared as distinctive peaks and are quantified using the Caliper data.

Anidulafungin is dissolved in DMSO and stored, and then diluted[2]. Stocks of CD101 (formerly SP 3025, biafungin, AF-025) are prepared fresh in 100% DMSO prior to use. The comparator antifungals Anidulafungin (ANF), Caspofungin (CSF), and Amphotericin B (AMB) are also prepared in 100% DMSO. MIC assays are performed via broth microdilution in accordance with CLSI guidelines, with the exception that test compounds are made up at a 50× final assay concentration and 100 μL assay mixture volumes are used (2 μL added to 98 μL of broth containing cells at 0.5×103 to 2.5×103 CFU/mL). All MIC assays are run at least three times, and a representative data set is shown. Quality control (QC) is assessed throughout the study via comparison of MIC values derived for WT C. krusei strain ATCC 6258 for AMB, CSF, and ANF with previously reported CLSI 24-h broth microdilution QC ranges[2].