α-Glucosidase-IN-32 (compound f26) is a reversible, noncompetitive and orally active α- glucosidase inhibitor with an IC 50 value of 3.07 μM. α-Glucosidase-IN-32 complex with α-glucosidase through hydrogen bonds and hydrophobic interactions, led to changes in the conformation and secondary strictures of α-glucosidase and further the inhibition of the enzymatic activity. α-Glucosidase-IN-32 can be used for diabetic disease research.