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Background: Hydrated fullerene C60 (HyFn) is a supramolecular object in which the nanosized fullerene molecule is enclosed in a multilayer shell of water molecules. Aqueous solutions of HyFn exhibit biological activity despite the fact that HyFn is chemically inert. Introduction and Rationale: It is known HyFn may act in low concentrations and that some of its activities may inversely depend on concentration. We questioned if HyFn could act on different biological test systems in ultra-high dilutions (UHD) and if HyFn UHD had peculiar physical-chemical properties. Methods: HyFn UHD were prepared by successive centesimal dilutions with succussion on each step of the original stock solutions of HyFn. Pure water used for dilutions and corresponding “dilutions” of water prepared in the same manner as HyFn UHD were used as controls. Results: HyFn UHD stabilized activity of different enzymes against denaturation, exerted cytostatic and cytotoxic action on cultured malignant cells, stimulated processes of respiration in whole human blood of healthy donors but attenuated the production of reactive oxygen species in blood of patients with chronic obstructive disease. Such effects of HyFn were expressed in UHD equivalent to 10-17 M and lower calculated “concentrations” of HyFn but not in higher calculated concentrations and in controls. HyFn UHD in calculated “concentrations” down to 10-31 M differed from respective controls in their UV spectra, in the rate of evaporation, they had significantly higher buffering capacity against acidification with HCl than controls. These properties fluctuated between consecutive dilutions of HyFn especially in the range of calculated concentrations 10–17–10–31 M. Conclusions: HyFn UHD express a wide spectrum of apparently beneficial biological activities. Even in the highest dilutions physical-chemical properties of active UHD differ from respective controls supporting the suggestion that these aqueous systems have specific structuredness and heterogeneity. HyFn UHD may be considered as prospective entities for their testing as homeopathic remedies. Keywords: Fullerene C60; ultra-high dilutions; physical-chemical properties; biological activity.