Azeliragon

• CAT Number: I004271
• CAS Number: 603148-36-3
• Molecular Formula: C32H38ClN3O2
• Molecular Weight: 532.12
• Purity: ≥95%
• Synonyms: 3-[4-[2-butyl-1-[4-(4-chlorophenoxy)phenyl]imidazol-4-yl]phenoxy]-N,N-diethylpropan-1-amine
• InChI: InChI=1S/C32H38ClN3O2/c1-4-7-9-32-34-31(25-10-16-28(17-11-25)37-23-8-22-35(5-2)6-3)24-36(32)27-14-20-30(21-15-27)38-29-18-12-26(33)13-19-29/h10-21,24H,4-9,22-23H2,1-3H3
• InChIKey: KJNNWYBAOPXVJY-UHFFFAOYSA-N
• SMILES: CCCCC1=NC(=CN1C2=CC=C(C=C2)OC3=CC=C(C=C3)Cl)C4=CC=C(C=C4)OCCCN(CC)CC

Azeliragon（Cat No.:I004271）is an orally active small-molecule antagonist of the receptor for advanced glycation end products (RAGE). It was developed as a potential therapeutic agent for Alzheimer’s disease and other neurodegenerative conditions. By blocking RAGE, azeliragon aims to inhibit inflammation, oxidative stress, and amyloid-β transport across the blood–brain barrier—processes linked to cognitive decline. Despite showing early promise in clinical trials, later-phase studies yielded limited efficacy, though research continues into its broader neurological and inflammatory applications. Azeliragon exemplifies a targeted approach to modulating neuroinflammatory pathways in chronic disease contexts.

Reference

[1]. Burstein AH, et al. Assessment of Azeliragon QTc Liability Through Integrated, Model-Based Concentration QTc Analysis. Clin Pharmacol Drug Dev. 2019 May;8(4):426-435.
[Content Brief]

[2]. Bongarzone S, et al. Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective. J Med Chem. 2017 Sep 14;60(17):7213-7232.
[Content Brief]

[3]. Chen Y, et al. RAGE ligation affects T cell activation and controls T cell differentiation. J Immunol. 2008 Sep 15;181(6):4272-8.
[Content Brief]