Aim To study the hypoglycemic effect and the mechanism of novel sulfonyluric compound G-003. Methods ① After compound G-003 was givenig for 7 days, the levels of fasting plasma glucose of normal mouse was assayed with glucose oxidase kit. ② Rat pancreatic islets, adipocytes and mouse heaptocytes were isolated and cultured. Effects of compound G-003 on insulin release, glucose transport and utilization and glycogen synthesis were studied. Results Compound G-003 markedly decreased the levels of fasting plasma glucose of normal mouse, stimulated isolated pancreatic rat islets to release insulin and increased glucose transport and utilization in isolated rat adipocytes. Compound G-003 has no effect on glycogen synthesis in isolated mouse hepatocytes. Conclusion Compound G-003 has a significantly hypoglycemic effect. The hypoglycemic mechanism of novel compound G-003 may be attributed to stimulate secretion of insulin and increase glucose transport and utilization.