Ciprofol (HSK3486), a novel short-acting intravenous anesthetic, is a positive allosteric regulator and direct agonist of γ-aminobutyric acid type A (GABAA) receptor. It is synthetized by introducing a cyclopropyl group in the isopropyl side chain of propofol. The incorporation of cyclopropyl not only increases the steric effect, but also the new chiral molecules formed introduce stereoselective effects, thereby increasing the affinity for GABA receptors. Ciprofol activates GABAARs, producing sedative or anesthetic effects. Ciprofol is expected to become the new choice for intravenous anesthetics due to its characteristics of high potency, rapid onset, rapid recovery, and fewer adverse reactions. It is suitable for sedation and general anesthesia in the endoscopy center, operating room, and intensive care unit. This review summarizes the pharmacological characteristics and clinical research progress of ciprofol.