All Photos(1)
Synonym(s):
PF-04494700, PF04494700, 3-(4-{2-Butyl-1-[4-(4-chlorophenoxy)-phenyl]-1H-imidazole-4-yl}-phenoxy)-propyl]-diethylamine 1, 3-[4-[2-Butyl-1-[4-(4-chlorophenoxy)phenyl]imidazol-4-yl]phenoxy]-N,N-diethylpropan-1-amine), PF 04494700, TTP 488, TTP-488, TTP488
Empirical Formula (Hill Notation):
C32H38ClN3O2
CAS Number:
Molecular Weight:
532.12
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
powder
color
, White to light brown
solubility
DMSO: 2 mg/mL, clear
storage temp.
room temp
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.
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.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective
Journal of Medicinal Chemistry, 60(17), 7213-7232 (2017)
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
The journal of prevention of Alzheimer's disease, 5(2), 149-154 (2018)
Melinda Magna et al.
NPJ breast cancer, 9(1), 59-59 (2023-07-14)
Triple-negative breast cancer (TNBC) is a highly aggressive and metastatic cancer subtype, which is generally untreatable once it metastasizes. We hypothesized that interfering with the Receptor for Advanced Glycation End-products (RAGE) signaling with the small molecule RAGE inhibitors (TTP488/Azeliragon and
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