Azeliragon

Research use only, not for human use.

An orally bioavailable small molecule inhibitor of RAGE.

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).

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. Cell Viability Assay Cell Line:Purified T cells from RAGE-/- or WT B6 mice.Concentration:4 nM Incubation Time:16 hours Result:Inhibited of WT but not RAGE-/- T cells, and significantly reduced the level of IFN-γ.

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). Animal Model:Prediabetic NOD/LtJ (6-7 week old) mice, NOD mice with spontaneous diabetes, WT BALB/c mice (8-10 week old) and B6 mice with diabetes .Dosage:100 mcg/d Administration:Intraperitoneal injection; every day Result:Prolonged islet auto and allograft survival.

TTP-488 | PF-04494700

Others

Other Targets

RAGE

Neurological Disease

Alzheimer Disease

603148-36-3

532.116

C32H38ClN3O2

>98% (HPLC)

10 mM in DMSO

CCCCC1=NC(=CN1C2=CC=C(C=C2)OC3=CC=C(C=C3)Cl)C4=CC=C(C=C4)OCCCN(CC)CC

1-Propanamine, 3-[4-[2-butyl-1-[4-(4-chlorophenoxy)phenyl]-1H-imidazol-4-yl]phenoxy]-N,N-diethyl-

(-20℃)

With Ice Pack

≥ 2 years