RAGE 229

Modify Date: 2025-07-28 13:00:16

RAGE 229 Structure
RAGE 229 structure
Common Name RAGE 229
CAS Number 2143072-85-7 Molecular Weight 386.45
Density N/A Boiling Point N/A
Molecular Formula C23H22N4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of RAGE 229


RAGE 229, N-(4-(7-cyano-4-(morpholin-4ylmethyl) quinolin-2-yl)phenyl)acetamide, 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].

 Names

Name RAGE 229

 RAGE 229 Biological Activity

Description RAGE 229, N-(4-(7-cyano-4-(morpholin-4ylmethyl) quinolin-2-yl)phenyl)acetamide, 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].
Related Catalog
Target

KD: 2 nM (ctRAGE); IC50: 26 nM (SMC migration)[1]

In Vitro RAGE229 has affinity for the ctRAGE with KDvalue of 2 nM and inhibits SMC migration with an IC50 value of 26 nM[1]. Cell Migration Assay [1] Cell Line: SMCs Concentration: 0.00006 -10 μM. Incubation Time: 1.5 h Result: Inhibited SMC migration with an IC50 value of 26 nM.
In Vivo RAGE229 (oral gavage, 5 mg/kg, twice daily, for 4 days) assuages short- and long-term complications of diabetes in mice. 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]. Animal Model: female CF-1 mice and male mice with diabetes[1] Dosage: 5 mg/kg Administration: oral gavage, 5 mg/kg, twice daily, for 4 days Result: Reduced inflammation score and infarct area in mice. Animal Model: C57BL/6J mice and BTBR ob/obmice[1] Dosage: 30, 10, and 3 mg/kg; 5 mg/kg Administration: 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 Result: Reduced the concentrations of CCL2, TNF-α and IL-6.
References

[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.

 Chemical & Physical Properties

Molecular Formula C23H22N4O2
Molecular Weight 386.45
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