Here, we extended our previous finding’s results and demonstrated that Sac-1004 inhibited IL-1β-induced endothelial permeability by stabilizing tight junction complexes, attenuated inflammation responses induced by IL-1β through inhibiting NF-κB activation, and significantly decreased neurological deficits, cerebral infarction, and glial activation in a rat model of transient focal cerebral I/R. The gene discussed is IL1B; the disease is cerebral infarction.