RAGE229 (RAGE-229) is a specific antagonist of ctRAGE-DIAPH1 interaction, high potently binds to cytoplasmic tail of RAGE (ctRAGE) with KD of 2 nM.
RAGE229 directly competes with DIAPH1 for RAGE binding, antagonizes the RAGE-DIAPH1 complex in a dose-dependent manner.
RAGE229 inhibits CML-AGE stimulated cultured smooth muscle cells (SMCs) migration with IC50 of 26 nM, shows no effect on PDGFBB-stimulated SMC migration.
RAGE229 also shows IC50 of 120 nM for inhibition of human SMC migration in primary human aortic SMCs.
RAGE229 assuaged short- and long-term complications of diabetes in both male and female mice, without lowering blood glucose concentrations.
RAGE229 reduced plasma concentrations of TNF-α, IL-6, and CCL2/JE-MCP1 in diabetic mice, in parallel with reduced pathological and functional indices of diabetes-like kidney disease in type 1–like diabetic C57BL/6J mice.
