AbstractAstragalus membranaceus Bungehas been used to treat numerous diseases for thousands of years. As the main active substance ofAstragalus membranaceus Bunge, astragalosideIV(AS‐IV) also demonstrates the potent protective effect on focal cerebral ischemia/reperfusion, cardiovascular disease, pulmonary disease, liver fibrosis, and diabetic nephropathy. Based on studies published during the past several decades, the current state ofAS‐IVresearch and the pharmacological effects are detailed, elucidated, and summarized. This review systematically summarizes the pharmacological effects, metabolism mechanism, and the toxicity ofAS‐IV.AS‐IVhas multiple pharmacologic effects, including anti‐inflammatory, antifibrotic, antioxidative stress, anti‐asthma, antidiabetes, immunoregulation, and cardioprotective effect via numerous signaling pathways. According to the existing studies and clinical practices,AS‐IVpossesses potential for broad application in many diseases.