Abstract: To study insulino-mimetic effects of bis(α-furancarboxylato)oxovanadium (IV) (BFOV), a orally active antidiabetic vanadyl complex, on glucose uptake and lipogenesis in isolated rat adipocytes were determined by using 2-deoxy-D-［³H］-glucose and D-［³H］-glucose, respectively. Lipolysis was assayed by free fatty acids (FFA) released from isolated rat adipocytes treated with epinephrine. The results showed that BFOV, similar to insulin, concentration-dependently significantly enhanced the uptake of 2-deoxy-D-［³H］-glucose and the transformation from D-［³H］-glucose to lipid in isolated rat adipocytes, with the EC₅₀ values of (0.31±0.08) mmol·L^-1 and (0.49±0.12) mmol·L^-1, respectively. Moreover, BFOV markedly inhibited FFA release from isolated rat adipocytes treated with epinephrine, and the IC₅₀ value was (0.30±0.20) mmol·L^-1. BFOV had insulino-mimetic effects such as enhancing glucose uptake and lipogenesis, as well as inhibiting lipolysis.