Azeliragon
An orally bioavailable small molecule inhibitor of RAGE; inhibits sRAGE from binding to RAGE ligands, S100b, amphoterin and carboxymethyl-lysine; has been shown to inhibit the binding of sRAGE to Aβ1-42 in a fluorescent polarization assay; reduces accumulation in the spleen of Aβ peptides and the expression of IL-6 and macrophage colony stimulating factor, reduces both inflammatory markers (TNF-α, TGF-β and IL-1) and CNS amyloid deposition.Alzheimer's Disease Phase 3 Clinical (In Vitro) :Azeliragon (4 nM; 16 hours; T cells) treatment inhibits of wild type mice (WT) but not the deletion of the receptor (RAGE-/- mice) T cells and significant reduction in the production of IFN-γ. (In Vivo) :Azeliragon (100 mcg/d; intraperitoneal injection; every day) treatment reduces syngeneic islet graft and islet allograft in NOD and B6 mice (Islets were isolated from young prediabetic NOD/LtJ mice and transplanted into NOD mice with spontaneous diabetes; islets were isolated from WT BALB/c mice and transplanted into B6 mice with diabetes) .
Product Specifications
CAS Number
603148-36-3
Product Name Alternative
TTP-488 | PF-04494700
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
CCCCC1=NC (=CN1C2=CC=C (C=C2) OC3=CC=C (C=C3) Cl) C4=CC=C (C=C4) OCCCN (CC) CC
Molecular Formula
C32H38ClN3O2
Molecular Weight
532.116
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1-Propanamine, 3-[4-[2-butyl-1-[4- (4-chlorophenoxy) phenyl]-1H-imidazol-4-yl]phenoxy]-N, N-diethyl-
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