Aquaporins (AQPs) are highly conserved small transmembrane proteins that facilitate the transport of water and small solutes across cell membranes. Aquaglyceroporin 7 (AQP7), a significant member of the AQP family, is widely distributed throughout the body. For years, AQP7 was predominantly recognized for its role as a small-molecule transporter, facilitating the passage of small molecular substances. However, growing studies have revealed that AQP7 is also involved in the regulation of lipid synthesis, gluconeogenesis, and energy homeostasis, and it is intimately linked to a variety of diseases, such as obesity, type 2 diabetes mellitus, cardiovascular diseases, cancer, and inflammatory bowel disease. This article presents a comprehensive overview of the structure of AQP7, its regulatory mechanisms, its vital roles in both healthy and diseased states, and potential therapeutic advancements. We hope that these studies will serve as a valuable reference for the development of future treatments and diagnostic protocols targeting AQP7.