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Submit ReviewRAGE 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.
Sold under license from New York University
分子量 | 386.45 |
公式 | C23H22N4O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2143072-85-7 |
PubChem ID | 132020228 |
InChI Key | VDYYVNHJRNDKDO-UHFFFAOYSA-N |
Smiles | N#CC=1C=CC=2C(=NC(=CC2CN3CCOCC3)C=4C=CC(=CC4)NC(=O)C)C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 38.65 | 100 |
以下数据基于产品分子量 386.45。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.59 mL | 12.94 mL | 25.88 mL |
5 mM | 0.52 mL | 2.59 mL | 5.18 mL |
10 mM | 0.26 mL | 1.29 mL | 2.59 mL |
50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
参考文献是支持产品生物活性的出版物。
Manigrasso et al (2021) Small-molecule antagonism of the interaction of the RAGE cytoplasmic domain with DIAPH1 reduces diabetic complications in mice. Sci.Transl.Med. 13 eabf7084 PMID: 34818060
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关键词: RAGE 229, RAGE 229 supplier, RAGE229, inhibitor, inhibits, interaction, receptor, for, advanced, glycation, end, products, RAGE, Diaphanous-1, DIAPH1, type, 1, 2, diabetes, anti-inflammatory, 7701, Tocris Bioscience
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Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.