Azeliragon，25MG，SML3972-25MG，Sigma

Biochem/physiol Actions

Orally active, brain-penetrant, selective receptor for advanced glycation end products (RAGE) antagonist in vitro and in vivo.


Azeliragon (PF-04494700; TTP488) is an orally active, brain-penetrant, selective receptor for advanced glycation end products (RAGE) antagonist (Kd = 12.7 nM using sRAGE; little affinity toward >100 receptors/transporters) that blocks known RAGE ligands binding (S100b, amphoterin, carboxymethyl-lysine, and Aβ1-42). Azeliragon (0.3-3 mg/kg/day p.o.) reduces brain amyloid (Aβ1-40 & Aβ1-42) and inflammatory markers (TNF-α, TGF-β and IL-1), while increases plasma Aβ in tgAPPSWE/LON mice, a mouse model with Swedish and London mutations that over-express human APP.