Azeliragon

SKU: orb1224503

Description

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).

Key Properties

• CAS Number: 603148-36-3
• MW: 532.116
• Purity: >98% (HPLC)
• Formula: C₃₂H₃₈ClN₃O₂
• SMILES: CCCCC1=NC(=CN1C2=CC=C(C=C2)OC3=CC=C(C=C3)Cl)C4=CC=C(C=C4)OCCCN(CC)CC
• Target: RAGE
• Solubility: 10 mM in DMSO

Bioactivity

• 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). 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.
• 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TTP-488 | PF-04494700

Quick Database Links

Gene Symbol

RAGE