Pain and inflammation are protective responses; however, when persistent, they can cause damage and reduce the quality of life. The limitations of current therapies underscore the importance of investigating new agents that are effective and have fewer adverse effects. Therefore, the present study aimed to evaluate the anti-inflammatory and antinociceptive activities of LASSBio-753 in rats. The animals were pretreated with LASSBio-753 at doses of 0.1, 1.0, and 10 mg/kg, p.o., and subjected to carrageenan-induced paw edema to determine the optimal dose for combating inflammation caused by this agent. Subsequently, paw edema was induced using inflammatory mediators: histamine, compound 48/80, serotonin, prostaglandin E2, and bradykinin. Carrageenan-induced peritonitis was induced to assess neutrophil migration, as well as the levels of TNF-α, IL-1β, myeloperoxidase, malondialdehyde, and glutathione in the peritoneal fluid. Acetic acid-induced abdominal writhing and formalin-induced paw licking were used to evaluate antinociceptive activity. The 10 mg/kg dose of LASSBio-753 demonstrated the best anti-inflammatory and antinociceptive effects, reducing carrageenan-induced edema and edema induced by inflammatory mediators, as well as reducing neutrophil migration, TNF-α and IL-1β, myeloperoxidase, and malondialdehyde, while preserving glutathione in the peritoneal fluid. In addition, it reduced the number of abdominal contractions and the duration of paw licking that were chemically induced. The results obtained demonstrate that LASSBio-753 possesses significant anti-inflammatory and antinociceptive potential and may be a promising candidate for the treatment of inflammatory diseases; however, studies in inflammatory disease models are needed to better elucidate its therapeutic potential.