Ascomycin(FK 520)

- Overview
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    Background
    
    Ascomycin (FK 520, FR900520) is a novel neutral macrolide immunosuppressant, isolated from the cultured broth of Streptomyces hygroscopicus subsp. yakushimaensis No. 7238.
    In vitro: Ascomycin (FK 520, FR900520) suppressed lymphocyte reaction in a dose dependent fashion. Ascomycin was non-toxic at concentrations less than 3,200 nM, at which the percent inhibition was 18.9%. Ascomycin showed antifungal activity against Aspergillus fumigatus IFO 5840. Ascomycin had no inhibitory effect on bacteria or yeast at 100 μg/ml [1].
    In vivo: Ascomycin was dose-dependently effective and clearly prolonged skin allograft survival at 3.2 mg/kg or more, though all skin allografts were rejected within 7 days in rats treated intramuscularly with olive oil. Ascomycin, dissolved in olive oil, showed no adverse effect when administered intraperitoneally to ddY mice (male, 8 weeks old) at 100 mg/kg [1].
    Clinical trial: Ascomycin macrolactam derivative, Pimecrolimus, had been tested in both adults and pediatric patients with Atopic Dermatitis in two seperate clinical trials.
    
    [1] Hatanaka H, Kino T, Miyata S, Inamura N, Kuroda A, Goto T, Tanaka H, Okuhara M. FR-900520 and FR-900523, novel immunosuppressants isolated from a Streptomyces. II. Fermentation, isolation and physico-chemical and biological characteristics. J Antibiot (Tokyo). 1988;41(11):1592-601.
- Properties
  - Categories
    
    Macrolide immunosuppressant, FK-520 analog
    
    Alternative Name
    
    Immunomycin;FK 520;FR 900520;FR-900520;FR900520;FK-520;FK520
    
    CAS Number
    
    104987-12-4
    
    Molecular Formula
    
    C43H69NO12
    
    Molecular Weight
    
    792.01
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥38.9 mg/mL in DMSO; insoluble in H2O; ≥98.6 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    SMILES
    
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    * For Research Use Only