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Azeliragon(PF-04494700,TTP488) — Datasheet

CAT. NO. DC8338

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ParameterValue
Chemical NameAzeliragon free base
CAS No.603148-36-3
Synonyms3--4--2-Butyl-1--4--4-chlorphenoxy-phenyl--1H-imidazol-4-yl-phenoxy--N-N-diethylpropan-1-amin;Azeliragon;1-PROPANAMINE, 3-[4-[2-BUTYL-1-[4-(4-CHLOROPHENOXY)PHENYL]-1H-IMIDAZOL-4-YL]PHENOXY]-N,N-DIETHYL-;TTP488;[3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-methanol;[3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethylamine;[3-(4-{2-butyl-1-[4-(4-chlorophenoxy)-phenyl]-1H-imidazole-4-yl}-phenoxy)-propyl]-diethyl-amine;3-(hydroxymethyl)phenylboronic acid pinacol ester;N-[3-[4-[2-Butyl-1-[4-(4-chlorophenoxy)phenyl]-1H-imidazol-4-yl]phenoxy]propyl]-N,N-diethylamine
FormulaC32H38ClN3O2
M.Wt532.125
SMILESClC1=CC=C(C=C1)OC2=CC=C(C=C2)N3C(CCCC)=NC(C(C=C4)=CC=C4OCCCN(CC)CC)=C3
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

TTP488 is an antagonist at the Receptor for Advanced Glycation End products, is evaluated as a potential treatment for patients with mild-to-moderate Alzheimer's disease (AD).

In Vitro

TTP488 is an orally active, centrally acting antagonist of RAGE-RAGE ligand interaction. Chronic oral dosing of TTP488 in AD transgenic mice led to a reduction of amyloid load in the brain, improves performance on behavioral testing and normalization of electrophysiological recordings from hippocampal slices.[1]

In Vivo

The small molecule RAGE antagonist, TTP488, is developed by Trans-Tech Pharma. The TTP488 or control peptide is administered i.p. daily at a dose of 100 mcg/d.[3] Successful use of the RAGE inhibitor TTP488 in Phase II testing has led to a Phase III clinical trial for AD patients.[2]

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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