产品
编 号:F749325
分子式:C23H22N4O2
分子量:386.45
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1mg
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5mg
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10mg
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生物活性:
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).

体内研究:
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.Animal Model:female CF-1 mice and male mice with diabetes
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
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.

体外研究:
RAGE229 has affinity for the ctRAGE with KDvalue of 2 nM and inhibits SMC migration with an IC50 value of 26 nM.
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