Azeliragon

Azeliragon is an orally bioavailable inhibitor of the receptor for advanced glycation endproducts (RAGE; K_d = 12.7 nM for human recombinant sRAGE), which transports amyloid-β (Aβ) from plasma into the CNS.¹ It is selective for sRAGE over greater than 100 receptors and transporters in a screening assay. Azeliragon (0.3, 1, and 3 mg/kg per day) prevents brain deposition of Aβ (1-40) (Aβ40) and Aβ42 in the APP/SWE/LON transgenic mouse model of Alzheimer’s disease and increases plasma Aβ levels when administered for three months starting at 12 months of age. In the same treatment paradigm, it dose-dependently reduces memory impairments in the Morris water maze compared with untreated control mice, decreasing the latency and distance traveled to the platform. Azeliragon (10 mg/kg) also increases cerebral blood flow in the hippocampus and frontal cortex in tgAPP/SWE/LON mice greater than six months old.

WARNING This product is not for human or veterinary use.

1. Burstein, A.H., Sabbagh, M., Andrews, R., et al. Development of azeliragon, an oral small molecule antagonist of the receptor for advanced glycation endproducts, for the potential slowing of loss of cognition in mild Alzheimer’s disease. J. Prev. Alzheimers Dis. 5(2), 149-154 (2018).