RAGE 229

• CAT Number: I043379
• CAS Number: 2143072-85-7
• Molecular Formula: C23H22N4O2
• Molecular Weight: 386.45
• Purity: ≥95%
• Synonyms: N-[4-[7-cyano-4-(morpholin-4-ylmethyl)quinolin-2-yl]phenyl]acetamide
• InChI: InChI=1S/C23H22N4O2/c1-16(28)25-20-5-3-18(4-6-20)22-13-19(15-27-8-10-29-11-9-27)21-7-2-17(14-24)12-23(21)26-22/h2-7,12-13H,8-11,15H2,1H3,(H,25,28)
• InChIKey: VDYYVNHJRNDKDO-UHFFFAOYSA-N
• SMILES: CC(=O)NC1=CC=C(C=C1)C2=NC3=C(C=CC(=C3)C#N)C(=C2)CN4CCOCC4

RAGE 229 is an orally active ctRAGE-DIAPH1 inhibitor. RAGE 229 can inhibit the intracellular RAGE signaling by inhibiting the interaction between the cytoplasmic tail of RAGE(ctRAGE) and Diaphanous-1(DIAPH1)[1].
RAGE229 has affinity for the ctRAGE with KDvalue of 2 nM and inhibits SMC migration with an IC50 value of 26 nM[1].
RAGE229 (oral gavage, 5 mg/kg, twice daily, for 4 days) assuages short- and long-term complications of diabetes in mice[1].
RAGE229 (oral or iv.; 150, 50 and 15 ppm chow; 30, 10, and 3 mg/kg per day per mouse) (5 mg/kg, ip. , every 12 hours for four total doses) reduces plasma concentrations of TNF-α, IL-6, and CCL2/JE-MCP1 in diabetic mice, and reduces pathological and functional indices of diabetes-like kidney disease[1].

Reference

[1]. Michaele B Manigrasso, et al. Small-molecule antagonism of the interaction of the RAGE cytoplasmic domain with DIAPH1 reduces diabetic complications in mice. Sci Transl Med. 2021 Nov 24;13(621):eabf7084.
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