| Identification | Back Directory | [Name]
Acetamide, N-[4-[7-cyano-4-(4-morpholinylmethyl)-2-quinolinyl]phenyl]- | [CAS]
2143072-85-7 | [Synonyms]
Acetamide, N-[4-[7-cyano-4-(4-morpholinylmethyl)-2-quinolinyl]phenyl]- | [Molecular Formula]
C23H22N4O2 | [MOL File]
2143072-85-7.mol | [Molecular Weight]
386.45 |
| Chemical Properties | Back Directory | [Boiling point ]
642.7±55.0 °C(Predicted) | [density ]
1.29±0.1 g/cm3(Predicted) | [solubility ]
DMSO:38.65(Max Conc. mg/mL);100.0(Max Conc. mM) | [form ]
Solid | [pka]
14.58±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
RAGE 229 is an antagonist of the interaction between the cytoplasmic tail of the receptor for advanced glycation end products (ctRAGE) and the formin, Diaphanous-1 (DIAPH1) (KD for binding to ctRAGE = 2 nM). RAGE 229 inhibits the migration of human aortic smooth muscle cells in an in vitro wound healing assay (IC50 = 120 nM). RAGE 229 reduces short- and long-term complications of diabetes in mouse models, without lowering blood glucose concentrations. RAGE 229 also reduces plasma concentrations of TNF-α, IL-6, and CCL2/JE-MCP1 and attenuates inflammatory signaling in diabetic mice. | [Uses]
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]. | [in vivo]
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]. | 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. |
| [storage]
Store at -20°C | [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. DOI:10.1126/scitranslmed.abf7084 |
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