RAGE 229 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。
| 生物活性 | RAGE 229 is an orally activectRAGE-DIAPH1inhibitor. RAGE 229 can inhibit the intracellular RAGE signaling by inhibiting the interaction between the cytoplasmic tail of RAGE(ctRAGE) and Diaphanous-1(DIAPH1)[1]. |
| IC50& Target | KD: 2 nM (ctRAGE); IC50: 26 nM (SMC migration)[1] |
体外研究
(In Vitro) | RAGE229 has affinity for the ctRAGE with KDvalue of 2 nM and inhibits SMC migration with an IC50value 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 IC50value of 26 nM. |
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体内研究
(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 BTBRob/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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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