Azeliragon

Azeliragon is an orally bioavailable inhibitor of the receptor for advanced glycation endproducts (RAGE, Kd = 12.7 nM for human recombinant sRAGE), which transports amyloid-beta (Abeta) from plasma into the CNS. 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 Abeta (1-40) (Abeta40) and Abeta42 in the APP/SWE/LON transgenic mouse model of Alzheimer's disease and increases plasma Abeta 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.Formal Name: 3-[4-[2-butyl-1-[4-(4-chlorophenoxy)phenyl]-1H-imidazol-4-yl]phenoxy]-N,N-diethyl-1-propanamine. CAS Number: 603148-36-3. Molecular Formula: C32H38ClN3O2. Formula Weight: 532.1. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS(pH7.2) (1:2): 0.33 mg/ml, DMSO: 1 mg/ml, Ethanol: 1 mg/ml. lambdamax: 266 nm. SMILES: CCCCC1=NC(C2=CC=C(OCCCN(CC)CC)C=C2)=CN1C3=CC=C(OC4=CC=C(Cl)C=C4)C=C3. InChi Code: 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. InChi Key: KJNNWYBAOPXVJY-UHFFFAOYSA-N.