化合物 RAGE 229 T61721

Product Introduction
Bioactivity


英文名: RAGE 229

描述: RAGE 229, N-(4-(7-cyano-4-(morpholin-4ylmethyl) quinolin-2-yl)phenyl)acetamide 是一种小分子 ctRAGE-DIAPH1抑制剂，具有口服活性。RAGE 229 可通过抑制 ctRAGE 与 DIAPH1 的相互作用来抑制细胞内 RAGE 信号。

体外活性: RAGE229 has affinity for the ctRAGE with K D value of 2 nM and inhibits SMC migration with an IC 50 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 IC 50 value of 26 nM.

体内活性: 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/ob mice [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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途