Anidulafungin-LY303366-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAnidulafunginCat. No.: HY-13553CAS No.: 166663-25-8Synonyms: LY303366分式: CHNO分量: 1140.24作靶點: Fungal作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 30 mg/mL (26.31 mM)* me

2、ans soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 0.8770 mL 4.3850 mL 8.7701 mL5 mM 0.1754 mL 0.8770 mL 1.7540 mL10 mM 0.0877 mL 0.4385 mL 0.8770 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建

3、議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.19 mM); Precipitated solution; Need ultrasonic2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.19 mM); Clear solution1/3 Master of Small Molecules 您邊的抑

4、制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Anidulafungin種新型的半合成棘球素，具有抗真 (antifungal) 效。IC50 & Target Antifungal 1體外研究 Anidulafungin (LY-303366) has MICs of 0.32 g/mL for all Candida albicans (n=99), Candida glabrata(n=18), and Candida tropicalis (n=10) isolates tested. Anidulafungin is also active agains

5、t Aspergillus species(minimum effective concentration at which 90% of the isolates are inhibited, 0.02 g/mL) (n=20), is lessactive against Candida parapsilosis (MIC at which 90% of the isolates are inhibited MIC90, 5.12 g/mL)(n=10), and is inactive against C. neoformans (MIC90 10.24 g/mL) (n=15) and

6、 B. dermatitidis (MIC90, 16 g/mL) (n=29).The MICs of Fluconazole for three strains of C. tropicalis, seven strains of C. glabrata, and twostrains of Candida krusei are 16 g/mL. The MICs of Anidulafungin for 11 of these 12 strains range from0.08 to 0.32 mg/mL. The twelfth strain is a C. krusei strain

7、 (Fluconazole MIC, 32 g/mL) for which theAnidulafungin MIC is 1.28 mg/mL. The MIC at which 90% of the isolates are inhibited (MIC90) for these 12strains is 0.32 g/mL. The Anidulafungin MIC90 for the remaining 18 C. glabrata isolates and C. tropicalisisolates for which the Fluconazole MICs are 8 g/mL

8、 is also 0.32 mg/mL. Anidulafungin appeares equallyactive against Candida species for which the fluconazole MICs are 16 mg/mL and against those for whichthe fluconazole MICs are 8 g/mL. Anidulafungin has significantly less activity against C. neoformans andB. dermatitidis than against C. albicans, C

9、. glabrata, and C. tropicalis. Ketoconazole and amphotericin B arethe most active antifungal agents tested for both C. neoformans and B. dermatitidis. Anidulafungindemonstrated potent in vitro activity against Aspergillus species with a MEC90 of 0.02 g/mL. MICs ofAnidulafungin for the control strain

10、 yeast isolates are 0.02 g/mL for C. albicans ATCC 90028, 0.16 mg/mLfor C. glabrata ATCC 90030, and 10.24 g/mL for C. neoformans ATCC 90112 1. Strains selected withCD101 that have a 2-fold or greater CD101 MIC increase also have at least a 2-fold MIC increase forAnidulafungin (ANF) and/or Caspofungi

11、n (CSF) 2.PROTOCOLCell Assay 2 Stocks of CD101 (formerly SP 3025, biafungin, AF-025) are prepared fresh in 100% DMSO prior to use. Thecomparator antifungals Anidulafungin (ANF), Caspofungin (CSF), and Amphotericin B (AMB) are alsoprepared in 100% DMSO. MIC assays are performed via broth microdilutio

12、n in accordance with CLSIguidelines, with the exception that test compounds are made up at a 50 final assay concentration and 100 L assay mixture volumes are used (2 L added to 98 L of broth containing cells at 0.5103 to 2.5103CFU/mL). All MIC assays are run at least three times, and a representativ

13、e data set is shown. Quality control(QC) is assessed throughout the study via comparison of MIC values derived for WT C. krusei strain ATCC6258 for AMB, CSF, and ANF with previously reported CLSI 24-h broth microdilution QC ranges 2.MCE has not independently confirmed the accuracy of these methods.

14、They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Clin Microbiol. 2017 Jun;55(6):1883-1893.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE mSphere. 2018 Nov 14;3(6). pii: e00547-18.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Zhanel GG, et al. In vitro activity of a new semisynthe

15、tic echinocandin, LY-303366, against systemic isolates of Candida species,Cryptococcus neoformans, Blastomyces dermatitidis, and Aspergillus species. Antimicrob Agents Chemother. 1997 Apr;41(4):863-52. Locke JB, et al. Characterization of In Vitro Resistance Development to the Novel Echinocandin CD101 in Candida Species. AntimicrobAgents Chemother.